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PHARMACOLOGY-FINALS

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PHARMACOLOGY FINALS

🩶
Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
- dissolves clots to ensure free
DRUGS AFFECTING THE BLOOD movement of blood through the
COAGULATION system

Blood Coagulation
DISORDERS AFFECTING BLOOD
Aka clotting, the process by
COAGULATION
which blood changes from
liquid to gel, forming a blood
clot
This leads to a decrease in
blood
CLOTTING PROCESS HEMORRHAGIC
A. Damaged vessel endothelium THROMBOEMBOLIC ● Excess
stimulates circulating platelets, ● Formation of bleeding
thrombi occurs
causing platelet adhesion.
results in ● Hemophilia
B. Platelets release mediators and
decreased ● Liver Disease
platelet aggregation results ● Bone Marrow
blood flow
Clot Resolution Disorders
through or
A. Anticlotting process total
● Antithrombin Ill (in plasma) and occlusion of a
rivaroxaban inhibit the activity of blood vessel
Stuart factor (factor Xa) and ● S/Sx: hypoxia,
thrombin anoxia, or
even necrosis
● Heparin enhances the activity of
in areas
antithrombin III.
affected by
● Dabigatran directly inhibits the
thrombin decreased
B. Fibrinolytic process blood flow.
● Clots are dissolve ● Coronary
Artery Disease

PLASMIN OR FIBRINOLYSIN
DRUGS AFFECTING CLOT FORMATION
AND RESOLUTION

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
I. ANTIPLATELET AGENTS tirofiban which are thru
Abciximab intravenously (IV)
Eptifibatide ● Dipyridamole is used orally or as
Anagrelide an IV agent.
Ticagrelor ● well absorbed and highly bound
Aspirin to plasma proteins.
Ticlopidine ● metabolized in the liver and
Cilostazol excreted in the urine
Tirofiban ● Can enter breast milk
Clopidogrel
Vorapaxar
Dipyridamole CONTRAINDICATIONS
- Presence of allergy
➔ Alter platelet aggregation and - Pregnancy
the formation of the platelet - During lactation
plug
CAUTIONS
INDICATIONS ● The presence of any known
● treat CV diseases that are prone bleeding disorder or active
to producing occluded vessels bleeding
● maintenance of venous and ● Recent surgery and closed head
arterial grafts injuries
● prevent cerebrovascular ● History of stroke, or transient
occlusion ischemic attack (TIA)
● as adjuncts to thrombolytic ● Anagrelide: with any history of
therapy in the treatment of thrombocytopenia
myocardial infarction (MI) ● Clopidogrel: for people who
● prevention of reinfarction after poorly metabolize a certain liver
MI. enzyme (CYP2C19)

PHARMACOKINETICS NURSING CONSIDERATION


● Are administered orally except ASSESSMENT (history & examination)
Abciximab, eptifibatide, and

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________

TEST MEASURE THE USES and ice → to decrease excessive blood


RAP
loss caused by anticoagulation.
EUT
IC • Mark the chart of any patient
RA
receiving this drug → to alert medical
NGE
staff that there is a potential for
aPT The activity of 1.5 Dosage
increased bleeding.
T the intrinsic -2. adjustment
• Offer support and encouragement →
PTT pathway of 5 for heparin,
to help the patient deal with the
coagulation ti low-molecul
m ar-weight diagnosis and the drug regimen
es heparins,
ba desirudin, II. ANTICOAGULANTS
sel argatroban, ● Interfere with the normal
in bivalirudin,
coagulation process by
e dabigratan,
interfering with the clotting
rivaroxaban
cascade and thrombin
INR Standardized 2- Warfarin formation
measure of 3.5 dose ● WARFARIN
prothrombin adjustments
● An oral drug
levels Fondaparin
● Causes a decrease in the
ux dose
adjustment production of vitamin
K-dependent clotting factors in
PT Time required 1.3 Warfarin
the liver → depletion of clotting
for clotting to -1. dose
factors and an extension of
occur 5 adjustments
extrinsic clotting times
pathway ● Adverse effects: Bleeding,
activity alopecia, dermatitis, bone
marrow suppression

IMPLEMENTATION DRUG TO DRUG INTERACTIONS WITH


• Provide increased precautions WARFARIN
against bleeding during invasive
Increase Decrease Increase
procedures: use pressure dressings
bleeding anticoagulat activity

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PHARMACOLOGY FINALS
Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )🩶
______________________________________________________________

effects ion and effects


of other BETRIXABAN
drug ● Factor Xa inhibitor, for
prevention of venous
Salicylates Barbiturates Phenytoin
Chloral hydrate Griseofulvin thromboembolism in
Phenybutazone Rifampin
disulfam Phenytoin
hospitalized patients at risk for
Oxyphenbutazone Glutethimide clotting
Thyroid drugs Carbamazepine
Glucagon Vitamin K
Danazol Vitamin E
Erythromyain Cholestyramine
Androgens Aminoglutethimid RIVAROXABAN AND EDOXABAN
Amiodarone e
● factor Xa inhibitors that stop the
Cetamandole Ethchlorvynol
Celotetan coagulation cascade
Mocalactam
Cefazoline ● for prevention of DVT (which
Cefoxitin might lead to PE), in patients
Ceftriakone
Famotidine undergoing knee or hip
Nalidixic Acid
replacement surgery
● for prevention of stroke in
ANTICOAGULANTS (Newer Oral Drugs) patients with nonvalvular AF
● for the prevention and
DABIGATRAN treatment of DVT and PE
● Directly inhibits thrombin
● Approved to reduce the risk of APIXABAN
stroke and systemic embolism • factor Xa inhibitor
in patients with nonvalvular • Caution: renal impairment
atrial fibrillation • approved for the treatment on
● Treatment of deep vein nonvalvular AF and the treatment of
thrombosis (DVT) and DVT and PE
pulmonary embolism (PE) in
patients treated with a DRUG-TO-DRUG INTERACTIONS WITH
parenteral anticoagulant for 5 NEW ORAL ANTICOAGULANTS
to 10 days
ALTERS Cause HIGHER
● Prevention of recurrence of DVT
METABOLISM of PLASMA LEVELS
and PE

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________

Dabigatran, of Betrixaban
Apixaban, - Amiodarone • Exogenous forms of naturally
Rivaroxaban, - Azithromycin occurring anticoagulants
Edoxaban - Verapamil
- Antifungals - Ketoconazole ANTITHROMBIN
- Erythromycin - Clarithromycin
• Interferes with the formation of
- Ritonavir
thrombin from prothrombin
- Phenytoin
- Rifampin • a naturally occurring anticoagulant

FONDAPARINUX
PHARMACOKINETICS
• inhibits factor Xa
• blocks the clotting cascade to
prevent clot formation
• Given via SQ
• Metabolized and excreted by the
kidneys

Note: not indicated use in patients with


artificial heart valves CONTRAINDICATIONS
- Presence of allergy
If suddenly stopped -> rebound - Pregnancy & lactation: oral
thromboembolic events
anticoagulants
- Hemorrhagic disorders, recent
HEPARIN, ARGATROBAN, AND
trauma, spinal puncture, GI ulcers,
BIVALIRUDIN
recent surgery, intrauterine device
• block the formation of thrombin from
placement, tuberculosis, presence of
prothrombin
indwelling catheters, and
• Given via IV
threatened abortion
• Excreted via urine
- Renal or hepatic disease

ANTITHROMBIN AND PROTEIN C


CAUTIONS
CONCENTRATE
- heart failure, thyrotoxicosis, senility or
• Replacement in specific genetic
psychosis, diarrhea or fever
deficiencies

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
HEPARIN control value or ratio of PT to INR of 2 to
• Inhibits thrombus and clot 3 → to evaluate the effectiveness of
production by blocking the the drug dose
conversion of prothrombin to • Evaluate for therapeutic effects of
thrombin and fibrinogen to fibrin heparin-whole-blood clotting time
(WBCT) of 2,5 to 3 times control or
• Does not enter breast milk activated partial thromboplastin time
(APTID of 1.5 to 3 times the control
USED FOR value → to evaluate the effectiveness
- acute treatment and prevention of of the drug dose.
venous thrombosis and PE
- treatment of AF with embolization ● Maintain antidotes on standby
- prevention of clotting in blood (protamine sulfate for heparin,
samples and in dialysis and venous vitamin K or prothrombin
tubing complex concentrate for
- diagnosis and treatment of warfarin) → in case of overdose.
disseminated intravascular ● Ensure a switch to another
coagulation (DIC) anticoagulant if apixaban,
edoxaban, dabigatran, or
Nursing Consideration: rivaroxaban is stopped suddenly
NURSING DIAGNOSES for any reason other than
• Risk for injury related to bleeding pathological bleeding →
effects and bone marrow effects because of the risk of
• Disturbed body image related to thromboembolic events.
alopecia and skin rash ● Monitor the patient carefully
• Ineffective tissue perfusion (total when any drug or herb is added
body) related to blood loss to or withdrawn from the drug
• Deficient knowledge of drug therapy regimen of a patient taking
warfarin → because of the risk of
IMPLEMENTATION drug-drug interactions that
• Evaluate for therapeutic effects of would change the effectiveness
warfarin-PT of 1.5 to 2.5 times the of the anticoagulant.

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
DRUGS AFFECTING CLOT FORMATION - cleared from body after liver
AND RESOLUTION metabolism
- can cross the placenta
I. THROMBOLYTIC AGENTS
Alteplase CAUTIONS
Reteplase - lactation
Tenecteplase
Urokinase ADVERSE EFFECTS
- Bleeding
CONTRAINDICATIONS - Cardiac Arrhythmias (with coronary
- Presence of allergy reperfusion
- Pregnancy - Hypotension
- recent surgery, active internal - Hypersensitivity reactions
bleeding, cerebrovascular accident
(CVA) within the last 2 months, UROKINASE
aneurysm, obstetrical delivery, organ Converts endogenous plasminogen to
biopsy, recent serious GI bleeding, plasmin → breaks down fibrin clots,
rupture of a non-compressible blood fibrinogen, and other plasma proteins
vessel, recent major trauma (including • Lyses thrombi and emboli
cardiopulmonary resuscitation), known • Used for lysis of PE or PE with unstable
blood clotting defects, cerebrovascular hemodynamics in adults
disease, uncontrolled hypertension
- hepatic disease ADVERSE EFFECTS
- Headache
• break down the thrombus that has - hypotension
been formed by stimulating the - bleeding
plasmin system (clot resolution) - bronchospasm
• Activates conversion of plasminogen - fever
to plasmin → breaks down fibrin - angioneurotic edema
threads and dissolves any formed clot - skin rash
- breathing difficulties
PHARMACOKINETICS - pain
- given via IV - anaphylactic shock

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
decrease excessive blood loss caused
Nursing Consideration: by anticoagulation.
ASSESSMENT (History & Examination) • Monitor coagulation studies regularly;
Assess for cautions or consult with the prescriber → to adjust
contraindications: the drug dose appropriately.
• any known allergies • Institute treatment within 6 hours
• pregnancy or lactation after the onset of symptoms of acute
• recent surgery MI → to achieve optimum therapeutic
• active internal bleeding effectiveness.
• cerebrovascular accident (CVA) • Evaluate the patient regularly for any
within the last 2 months sign of blood loss (petechiae, bleeding
• aneurysm gums, bruises, dark-colored stools,
• obstetrical delivery dark-colored urine) → to evaluate the
• organ biopsy effectiveness of the drug dose
• recent serious GI bleeding and to determine the need to consult
• rupture of a noncompressible blood with the preseriber if
vessel bleeding becomes apparent.
recent major trauma (including • Arrange to type and crossmatch
cardiopulmonary resuscitation) blood in case of serious blood
• known blood clotting defects Loss that requires whole-blood
• cerebrovascular disease transfusion.
• uncontrolled hypertension • Monitor cardiac. rhythm continuously
if the drug is being given for acute MI
→ because of the risk of alteration in
cardiac function; have life support
equipment on standby as needed,
IMPLEMENTATION
• Provide increased precautions LOW-MOLECULAR-WEIGHT HEPARINS
against bleeding during invasive inhibit thrombus and clot formation by
procedures; use pressure dressings blocking factors Xa and lla
and ice avoid IM injections; and do not • do not greatly affect thrombin,
rub subcutaneous injection sites → to clotting, or the PT → fewer systemic
adverse effects

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
• block angiogenesis ANTIDOTES
• preventing clots and emboli VITAMIN K
formation after certain surgeries or • reverse the effects of warfarin →
prolonged bed rest. normalize clotting time
• given just before (or just after) the • promotes the liver synthesis of
surgery and is continued for 7 to 14 several clotting factors
days during the postoperative • anticoagulant-induced prothrombin
recovery process deficiency
• Caution: avoid combining these - 2.5 to 10 mg intramuscularly (IM) or
drugs with standard heparin subcutaneously or, rarely, 25 mg IM or
subcutaneously
III. ANTICOAGULANT ADJUNCTIVE
THERAPY FRESH FROZEN PLASMA
Lepirudin • For patients bleeding excessively and
Protamine Sulfate for faster response
Prothrombin Complex Concentrate
Vitamin K PROTHROMBIN COMPLEX
CONCENTRATE
LEPIRUDIN • a blood product, infused IV to supply
directly inhibits thrombin, blocking the the clotting factors needed to restore
thromboembolic effects of this hemostatic balance
reaction • dosing is based on the patient's INR
• developed to treat a rare allergic
reaction to heparin (heparin-induced PROTAMINE SULFATE
thrombocythemia with associated • antidote to heparin overdose
thromboembolic disease) • A dose of 1 mg IV protamine
• 0.4-mg/kg initial IV bolus followed by neutralizes 90 units of heparin derived
a continuous infusion of 0.15 mg/kg for from lung tissue or 110 USP of heparin
2 to 10 day derived from the intestinal mucosa
• Monitor for: bleeding from any site • must be administered slowly, not to
and for the development of direct exceed 50 mg IV in any 10-minute
hepatic injury period

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
• Can cause potentially fatal I. ANTIHEMOPHILIC AGENTS
anaphylactic reactions Antihemophilic Factor
Antihemophilic Factor Fc Fusion Protein
PENTOXIFYLLINE Antihemophilic Factor Porcine
drug that can induce hemorrhage Sequence
decreases platelet aggregation and Antiinhibitor Coagulant Complex
decreases the fibrinogen Coagulation Factor Viiafactor IX
concentration in the blood Factor IX Complex
• decrease blood clot formation and Factor XIII Concentrate
increase blood flow through narrowed
or damaged vessel ● replace clotting factors that are
• effective in treating intermittent either missing or low in a
claudication particular hemophilia
• Adverse effects: headache, dizziness,
nausea, and upset stomach PHARMACOKINETICS
• Taken orally three times a day for at - given IV
least 8 weeks - Trz: 24-36 hours
CONTRAINDICATIONS
BLEEDING DISORDERS - the presence of known allergy to

HEMOPHILIA LIVER BONE mouse proteins


DISEASE MARROW - FACTOR IX: presence of liver disease
DISORDERS
with signs of intravascular coagulation
A genetic The clotting Platelets are or fibrinolysis
lack of factors and not formed in
- Coagulation Factor VIla: known
clotting proteins sufficient
factors needed for quantity to allergies to mouse, amster, or bovine
leaves the clotting are be effective products
patient not produced
vulnerable to - Pregnancy &
excessive lactation
bleeding with
• Normal plasma protein that is
any
Inur needed for the transformation of
prothrombin to thrombin

DRUGS USED TO CONTROL BLEEDING • Treatment of classic hemophilia →


provide temporary replacement of

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
clotting factors to correct or prevent - weakness
bleeding episodes or to allow - hypotension
necessary surgery - nausea
• Ti/2: 12 hours, cleared from the body - cramps
by normal protein metabolism - diarrhea
- fertility problems
ADVERSE EFFECTS - malaise
- Allergic reaction - elevated serum creatine
- stinging at the injection site phosphokinase
- headache
- rash DRUG-DRUG INTERACTIONS
- chills - development of hypercoagulation
- nausea states if it is combined with oral
- hepatitis contraceptives or estrogen
- AIDS (risks associated with the use of - risk for bleeding increases if it is given
blood products) with heparin

AMINOCAPROIC ACID TOPICAL HEMOSTATIC AGENTS


CONTRAINDICATIONS used to care for wounds or decubitus
- Allergy to the drug ulcers
- Acute DIC
PHARMACOKINETICS
CAUTIONS - Absorbable gelatin and
- allergy microfibrillar collagen: sponge form,
- cardiac disease applied directly to the injured area
- renal & hepatic dysfunction until the bleeding stops
- pregnancy - Human fibrin sealant: spray form
- lactation and apply in a thin layer onto the graft
bed
ADVERSE EFFECTS - Thrombin: from bovine sources,
- dizziness applied topically and mixed in with the
- tinnitus blood
- headache

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
- Thrombin recombinant: applied ● Urinalysis and clotting studies
directly to the bleeding site surface in ● Renal and hepatic function test
conjunction with an absorbable gelatin
sponge NURSING DIAGNOSES
● Disturbed sensory perception
CAUTIONS related to CNS effects
- allergy to bovine products ● Acute pain related to GI, CNS, or
- children skin effects
ADVERSE EFFECTS ● Deficient knowledge of drug
- pose a risk of infection therapy

Nursing Consideration: PLANNING


ASSESSMENT (History & Examination) • The patient will receive the best
therapeutic effect from the drug
Assess for cautions or therapy.
contraindications: • The patient will have limited adverse
● any known allergies to the drugs effects to the drug therapy.
● Acute DIC • The patient will have an
● Renal & hepatic dysfunction understanding of the drug therapy,
● Lactation adverse effects to anticipate, and
measures to relieve discomfort and
Assess baseline status before improve safety.
beginning therapy
● body temperature IMPLEMENTATION
● skin color, lesions, and • Monitor the patient for any sign of
temperature affect, orientation, thrombosis → to arrange to use
and reflexes comfort and support measures as
● pulse, blood pressure, and needed (eg, support hose, positioning,
perfusion ambulation, exercise).
● respirations and adventitious • Orient the patient and offer support
sounds and safety measures if hallucinations
● Bowel sounds and normal or psychoses occur → to prevent
output patient injury.

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
• Offer comfort measures → to help the Monitor the effectiveness of comfort
patient deal with the effects of the measures and compliance with the
drug. These include small, frequent regimen.
meals, mouth care, environmental
controls, and safety measures. DOSAGE CALCULATIONS
• Monitor clinical response and clotting
4 measuring system
factor levels regularly → arrange to
1. Metric System
adjust dose as needed.
● most widely used
• Provide thorough patient teaching
● Based on the decimal
• name of the drug, dosage prescribed
system
measures to avoid adverse effects
● Determined as multiples
warning signs of problems
of 10
• the need for periodic monitoring and
● 1995, established
evaluation → to enhance patient
standards, requiring that
knowledge about drug therapy and to
all prescriptions may be
promote compliance with the drug
dispensed only in this
regimen.
system
• Offer support and encouragement →
● MOST ACCURATE
to help the patient deal with the
● Developed 18th century
diagnosis and the drug regimen.
● Most internationally
accepted
EVALUATION
• Monitor patient response to the drug
(control of bleeding episodes, BASIC UNIT OF MEASURE are

prevention of bleeding episodes)


Gram (G, g, For weight
• Monitor for adverse effects
gm)
(thrombosis, CNS effects, nausea,
hypersensitivity reaction, hepatitis, Liter (L) For volume
AIDS).
Meter (m,M) For Length
• Evaluate the effectiveness of the
teaching plan (patient can name drug.
Prefix indicate the side of unts in
dosage, adverse effects to watch for,
multiples of 10 kilo, is the prefix
and specific measures to avoid them).

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PHARMACOLOGY FINALS
🩶
Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
used for larger units while the
smallest METRIC EQUIVALENT
1 gram = 1000mg = gr 15-16
METRIC UNITS = used in most 0.5 = 500mg = gr 7.5
drug notations 0.3 gm = 300mg = gr5
0.1gm = 100
1gm = 1000mg
1L = 1000mL 2. Apothecary system
1mg = 1000mg
● Used in England since the 17th
The rule for Metric conversion century
● Very old system
a. When covering LARGER units to ● Used by
SMALLER units in a metric apothecaries/pharmacists
system, move the decimal point
3 places to the RIGHT THE BASIC UNIT OF MEASURE ARE:

1 kilometer =1.0>0>0 liter MINIM = for liquid measure


Hence 1kl = 1000 liters GRAIN = for solid

1 kilogram = 1.>0>0> 0 grams ● The system used ROMAN


1kg = 1000gm numerals placed after th unit of
measure to denote amount
b. When converting SMALLER units
to LARGER units more the Ex: 15gr (gr xv)
decimal point 3 places to the
LEFT RULE FOR APOTHECARY CONVERSION
A. When converting LARGER units to
Example: Change 1000mg to grams SMALLER UNITS, multiply the
measurement that is requested
1000mg= 1<0<0<0 gm by the basic equivalent value

Hence, 1000mg is 1gm E.g 3 fluid ox = ______

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PHARMACOLOGY FINALS
🩶
Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
Fluid dram convert 3qt
G (from latin granum)
Given 1 fluid oz =8 fluid dram Drop abbreviated as gtt (guttae)

Hence fl oz, 8fl dram = 24 fl


dram pints FLUID VOLUME
1 pint =16 fluid oz
Given: 1gt =2 pints 1 quart = 2 pints
1fL oz = 8 drains
3gt x 2pints =6 1fL gram = 60 minim = 4 minim
1 minim = 1 drop (gtt)
B. when converting SMALLER to 1 cc = 15-16 mins
LARGER units divide the request
no. by the equivalent value Minims used in eye/ear medications

E.g 8fl oz = _____ pint 3. HOUSEHOLD SYSTEM


● Measuring system that is found
Given:1 pint = gl oz in recipe books commonly used
in home or community setting
Hence: ● Measurement is approximate
8fl oz divided by 16 = 0.5 or ⅕ pint and not as accurate as the
_ grams metric system
Oz = 3 3
THE BASIC UNITS OF MEASURE ARE
DRY WEIGHT
Teaspoon - the basic unit of fluid
1 ounce (oz) 480 grains
measure
1 ounce (oz) 8 grains Pound - the basic unit of solid measure

1 drain 60 grains
HOUSEHOLD EQUIVALENT
1 scruple 20 grains
1 cup = 8 oz
1 glass = 8 oz
Note: 1 coffee cup = 60z

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
1oz = 2 tbsp = 30ml ● Is another older system that was
1pound (Ib) = 16 oz very popular when pharmacists
1 tsp =5ml = 60 gtts routinely had to compound
1 tbsp = 3 tsp medications
1 gtt =1 minim ● Not used much in the hospital
1cc = 1ml but is still used by
manufacturers
1tbsp = 5ml
cc&ml = same (Note: 10 units = 30 days - insulin)

● The system uses ounces and


RULE OF CONVERSION
grains but they measure
A. Converting larger units to
differently than the apothecary
smaller units, multiply by the
and household systems. It is
number by the basic equivalent
seldom.
value
● Used by the prescriber but may
be used for bulk medicines
Example : 2 glasses = _____ oz coming from the manufacturer

Given: 2 glasses x 8oz


5. OTHER SYSTEM
1 glass
8 oz = 16 oz
● Unit = reflects the biological
activity of the drug in m1l of
B. Converting SMALLER to LARGER
solution
units divide the number by the
● The unit is unique for the drug
equivalent value
that measures a unit of heparin
is not comparable with a unit of
Example : 6 tsp = ______ tsp
insulin

Given: 6/3 = 2 tbsp


6 tsp = 3tsp (divide) Milliequivalents (mEq)

● Are used to measure


electrolytes (e,g,k,Na, Ca,
4. AVOIRDUPOIS SYSTEM

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
fluoride) the milliequivalents processed by the liver as
refer to the ionic activity of the lipoproteins (VLDL → IDL)
drug
● HDL = good cholesterol
● LDL = bad cholesterol -build up
International units are sometimes used
of lipids in blood has (HMC Coa
to measure certain vitamins or
Re autase, helps increase bad
enzymes and are also unique to each
cholesterol levels)
drug

NORMAL VALUES
Interpreting drug labels
Pharmaceutical companies usually Good Cholesterol (HDL)
label their drugs with the brand name,
Male: Female:
also the trade name and generic.
35-65 35-80
miligram-liter miligram-liter
LIPID-LOWERING DRUGS
Bad Cholesterol (LDL)
● Drugs that lower levels of
Less than a 100 miligram per liter
cholesterol
● Consume food high in dietary
fats Build up of lipids in blood →

● Broken down in the stomach Progressive growth of atheroma in the

into fatty acids, lipids and coronary arteries (myocardial

cholesterol infarction) → injury in the endothelial

● Gall bladder contracts the lining of the arterial wall →

release of bile acids ( they inflammatory reaction is initiated

breakdown fats to be micelles, platelets, fibrin, fat, collect on the

and these are packed into injured

chylomicrons in the small


intestine → chylomicrons 1. Bild Acid Sequestrants

through the small intestine →go ● Bind with bile acids in the

into circulation →broken down intestine to form insoluble

to be used as energy and complex → bile acids is


used up cholesterol is

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PHARMACOLOGY FINALS
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Reviewer ni Mai (pls dont attack me if may kulang, GOODLUCK FUTURE RNS )
______________________________________________________________
excreted → stored 1. Assess contraindications and
cholesterol in the liver is allergy
processed to make more 2. Inspect for skin color
bile acids → hepatic 3. Perform physical assessment
intracellular cholesterol 4. Assess bowel elimination
level fails (auscultate bowel sounds)
● SAFEST 5. Assess neurological status
● Prefix: choles- 6. Monitor results of Lab results

Examples: Note: if px LDL increase - advice to not

1. Colesevelam only drink during their admission

2. Colestipol
3. Cholestyramine - Diagnose: Constipation r/t GI effects

prepared in
powdered form Note:
● Mix powder form w/ fruit juice,
liquids, cereals and pulpy fruits
● If tablet, advice px to not chew, cut
Contraindications and digest the whole tab
● Biliary obstruction
● allergy
Interactions
Caution ● Malabsorption of fat-soluble
● Intestinal problem vitamins
● Pregnant
C Corticosteroids,
Adverse Effect DD Diuretics,
● CNS - headache, muscle pain, HH Hormone and
anxiety W Hormonal
● GIT - fecal impaction, nausea, Contraceptives
constipation, hemorrhage and Warfarin

Oral - 1 hour before or 4-6 hours before


Note: advice patient to increase fluid and fiber
(increase FF) meal (para makasama sa food)

ASSESSMENT

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● Administer other oral
medications 1 hour before or 4-6 Check lipid
hours of bile acids to avoid
GI effects
drug-to-drug interactions
Monitor px
ADVERSE EFFECTS
Rhabdomyolysis
2. HCDG COA Reductase Inhibitors
(breakdown of
● Bff ni LDL
muscle and leads
● Hydroxy Methyl Glutanly - Co to renal failure)
enzyme Reductase Inhibitors

Block HCDG COA Reductase → Block


Atorvastatin,
synthesis of cholesterol in the liver lovastatin,
(and also degrades) → lower simvastatin
+grapejuice
cholesterol and LDL levels
increase serum
levels and increase
- statin (suffix) INTERACTIONS the risk of toxicity
Atorvastatin (DO NOT
ADMINISTER)
Rosuvastatin
Sinvastin Erythromycin,
ketoconazole, HIV
pro inhibitors,
PHARMACOKINETICS
cyclosporine, and
● Distributed in the liver ezetimibe can
● Absorbed in the GIT increase levels
● Metabolized in the liver

NOTE: Statins are given at night ( most


Administer the
cholesterol is synthesized when dietary drug daily as
intake is at its lowest.) ordered by a
doctor with or
INTERVENTIONS without food
High-intensity statin - can be given
during the day (50%) Advice
1. Atorvastatin contraceptives
2. Rosuravastin used during

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pregnancy
Statins + Ezetimibe = increase risk of
Levatratin,
myopathy and liver disease
atorvastatin may
cause renal failure

Contraindications
3. Cholesterol Absorption
● Allergy
● Liver impairment
Works in small
intestine → Less
Cautions
dietary
cholesterol is ● Pregnancy
Ezetimibe
delivered to the
liver → Increases Adverse effects
clearance of ● Diarrhea
cholesterol in the
● Rare cases can lead to hepatitis
liver → Liver
● Respiratory tract infection
increase
clearance
INTERVENTION
● Encourage the patient to
INTERACTIONS
follow lower
Ezetimibe + statins = lower total and
lower-cholesterol diet
LDL cholesterol
4. PCSK Inhibitor (binds, LDL,
increases LDL levels)
Ezetimibe + fenofibrate = lower
cholesterol and triglycerides
Suffix: mab
Alirocumab
Bile acid Seq + Ezetimibe =
Evulucumab
interference with absorption of
Ezetimibe
→ binds to PCSK9 enzyme and
inhibits attachment to the LDL
Warfarin + Ezetimibe = increase level
receptor (in the liver cell) →
of warfarin (check px for signs of
more LDL is processed by the
bleeding)

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liver → decreased level of LDL in
the plasma

CONTRAINDICATIONS
● Allergy
● Latex allergy

CAUTIONS
● Pregnancy

ADVERSE EFFECT
● Urinary tract infection (UTI)
● Nasopharyngitis
● URTI
Influenza

Note: monitor px for signs of infection

5. Other lipid-lowering agents

1. Fibrates
2. Vitamin B3
3. Omega 3 fatty acid - lower
triglyceride levels
4. Other therapies

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- Can develop

DRUGS AFFECTING THE GI TRACT gynecomastia and


galactorrhea and it

I. Drugs used to treat inhibits the


metabolism of drugs
Gastroesophageal Reflux and Ulcer
2. Famotidine
Disease
- Oral and parenteral
Histamine - the regulator of
- Metabolized in liver
- allergy
- Half-life: 2.5-3.5h
- Immune response
- Gastric secretion
- Excreted in the urine

- sleep/wake, cognition - It is approved for use


in children aged 1-16

H1 - are available for allergy treatment, - Crosses the placenta


vasodilation, bronchoconstriction, mucus and human milk
secretion 3. Nizatidine
H2 - gastric acid secretion
- Oral
H3 - CNS
- Metabolized in Liver
H4 - immune response modulation
- Half-life: 1-2 hours
- Approved for px
● The drugs used to treat GERD
with liver or kidney
and ulcer disease include
dysfunction
histamine-2 antagonists, which
- Crosses the placenta
block the release of hydrochloric
and human milk
acid in response to gastrin

● Oral formulations of these


HISTAMINE-2 ANTAGONISTS
medications are available as
● Blocks the release of
OTC medications.
hydrochloric acid in response to
gastrin ● Allergy to any
drugs of this
● This drug include class to
1. Cimetidine prevent
hypersensitivity
- Oral
reactions
- Metabolized in liver ● Pregnancy or
- Half-life: 2 CONTRAINDICATIONS lactation
AND CAUTIONS ● Hepatic and
- 1st developed

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renal - Hormonal effects


dysfunction (gynecomastia,
● Care should impotence with
also be taken if cimetidine)
prolonged or
continual use
of these drugs NURSING CONSIDERATIONS
is necessary
because they
may be 1. ASSESSMENT (HISTORY AND
masking EXAMINATION)
serious
underlying
A. Assess for allergies to H
conditions antagonists, impaired renal or
hepatic function, detailed Gl
history, and pregnancy or
- Headache lactation status to identify
- Dizziness potential contraindications or
- Diarrhea or
SIDE EFFECTS constipation
risks.
- Nausea B. Conduct a physical
- fatigue
examination, including skin
inspection, neurological and
- Allergic reactions
cardiopulmonary evaluation,
(rash, swelling,
difficulty and abdominal assessment, to
breathing) establish baselines, monitor
- Confusion,
agitation,
therapy effectiveness, and
hallucinations detect adverse effects.
(especially in
C. Regularly monitor liver and renal
LONG TERM AND older adults)
SERIOUS ADVERSE - Liver damage function tests to adjust dosages
EFFECTS (yellowing if necessary and ensure safe
skin/eyes, dark
urine)
drug metabolism and excretion.
- Blood disorders
(low white blood
INTERVENTION WITH RATIONALE
cells, platelets, or
anemia)
- Kidney issues 1. Timing of Administration: Administer
(acute kidney
injury) the oral drug with meals or at bedtime

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to ensure therapeutic levels when administration schedule, importance
needed most. of timing, access to bathrooms, signs
2. Dose Adjustment: Reduce the dose of adverse effects, safety measures,
in patients with hepatic or renal adherence to therapy, and the need
dysfunction to prevent toxicity. for regular monitoring and evaluation
to enhance understanding and
3. Drug Interaction Monitoring: compliance with the treatment plan.
Carefully assess for potential
drug-drug interactions, especially with ANTACIDS
cimetidine, due to its effects on liver ● Antacids are a group of
enzymes. inorganic chemicals that
neutralize stomach acid.
4. Patient Comfort: Provide comfort ● Antacids are available OTC, and
measures such as analgesics, many patients use them to
bathroom access, and assistance with self-treat a variety of Gl
mobility to reduce adverse effects. symptoms.
● The choice of antacid depends
5. Patient Safety: Periodically reorient on adverse effects and
the patient and implement safety absorption factors.
measures if central nervous system ● Available agents are sodium
(CNS) effects occur to ensure safety bicarbonate (generic), calcium
and improve tolerance. carbonate (Oystercal, Tums,
and others), magnesium salts
6. Follow-Up Care: Schedule regular (Milk of magnesia), and
follow-ups to evaluate drug efficacy aluminum salts (Ampphojel and
and the underlying condition others).

7. Emotional Support: Offer support THERAPEUTIC ACTIONS AND


and encouragement to help patients INDICATIONS
manage their disease and treatment. Antacids neutralize stomach acid by
direct chemical reaction. They are
8. Patient Education: Teach patients recommended for the symptomatic
about the drug's name, dosage,

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relief of upset stomachs associated hypersensitivity
with hyperacidity, as well as reactions.

hyperacidity associated with peptic


Caution should be used
ulcer, gastritis, peptic esophagitis, in the following
gastric hyperacidity, and hiatal hernia. instances:
● Any condition
that can be
PHARMACOKINETICS
exacerbated by
electrolyte or
SODIUM CARBONATE acid-base
Types of preparation: Baking Soda imbalance

Powder, Tablet, Solutions, and ● Renal


dysfunction,
Injectables
which could
Peak Level: 1-3 hours lead to
Excreted: Urine electrolyte
CAUTIONS disturbance if
any absorbed
Crosses the placenta and human milk.
antacid is not
neutralized
ALUMINUM SALT properly
Types of preparation: tablet, capsules, ● Any Electrolyte

suspensions and liquids imbalance,


which could be
Metabolized: Liver
exacerbated by
Excreted: Feces the
electrolyte-cha
Do not cause acid rebound BUT are nging effects of
these drugs
not very effective in neutralizing acid.
● Gl Obstruction,
which could
Antacids are cause systemic
contraindicated in the absorption of
presence of any known the drugs and
allergy to antacid increased
products or any adverse effects
CONTRAINDICATIONS
component of the drug ● Pregnancy and
to prevent lactation,

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because of the ASSESSMENT: HISTORY AND


potential for EXAMINATION
adverse effects ● Assess for possible contained to
on the fetus or
tiene or cautions: any history of
neonate
allergy to anaton, to event
hypersensitivity reactions, renal
dysfunction, which might
ADVERSE EFFECTS
interfere with the excretion of
• Disruptions in acid-base and
the drug; electrolyte
electrolyte balance.
disturbances, which could be
• Frequent use can lead to acid
exacerbated by the effects of
rebound, where increased stomach
the drug: and current status of
acid is produced, creating a cycle of
pregnancy or lactation due to
excessive antacid consumption.
possible effects on the fetus or
• Systemic effects: such as alkalosis,
newborn.
causing symptoms like nausea,
vomiting, neuromuscular changes,
INTERVENTION WITH RATIONALE
headaches, and even coma.
1. Administer the drug apart from
• Specific antacids have additional
any other oral medications
risks: calcium salts can cause
approximately 1 hour before or 2
hypercalcemia (high calcium level in
hours after to ensure adequate
blood serum) and milk-alkali
absorption of the other
syndrome (high calcium level in the
medications.
body), aluminum salts can lead to
2. Have the patient take
hypophosphatemia (electrolytes
medications as instructed on
disorder in a low level of phosphate in
label. Some tablets need to be
the blood), and sodium bicarbonate
chewed thoroughly and
can cause fluid retention and heart
followed with water to ensure
failure due to its high sodium content.
that therapeutic levels reach the
stomach to decrease acidity.
NURSING CONSIDERATIONS FOR
3. Assess the patient for any signs
PATIENTS RECEIVING ANTACIDS
of acid-base or electrolyte
imbalance to ensure early

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detection and prompt - Half-life of 2 hours,
interventions duration of 12 hours.
4. Monitor the patient's nutritional 4, Pantoprazole and rabeprazole
status if diarrhea is severe or - Half-lives of 90 minutes,
constipation leads to decreased durations of 12-14 hours.
food intake, to ensure adequate 5. Dexlansoprazole
fluid and nutritional intake and - Delayed capsule with two
promote healing and GI stability. releases, peaks at 1-2 hours and
4 hours, offering extended
PROTON PUMP INHIBITORS protection.
Suppress the secretion of hydrochloric
acid into the lumen of the stomach. Pregnancy and Lactation:
Six proton pump inhibitors are - No adequate studies on whether
available: these drugs cross the placenta or
omeprazole (Prilosec), enter human milk.
esomeprazole (Nexium),
lansoprazole (Prevacid), INDICATION
dexlansoprazole SHORT TERM TREATMENT
(Dexilant), pantoprazole (Protonix), ● Active duodenal ulcers
and ● Gastroesophageal reflux
Frabeprazole (Aciphex). disease (GERD)
● Erosive esophagitis
PHARMACOKINETICS ● Benign active gastric ulcers
1. Omeprazole
- Faster acting, rapidly LONG TERM TREATMENT
excreted, half-life of ● Pathological hypersecretory
30-60 minutes. conditions:
2. Esomeprazole ● Zollinger-Ellison Syndrome
- Longer-acting, half-life of ● Chronic Gastritis
60-90 minutes, duration ● Maintenance therapy for
of 17 hours, metabolized healing erosive esophagitis and
slower than omeprazole. ulcers
3. Lansoprazole

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COMBINATION THERAPY 4. Skin Reactions: Rash, hair loss
● Treatment of Helicobacter pylori (alopecia), itching (pruritus), dry
infection (with amoxicillin and skin, and back pain.
clarithromycin) 5. Other Symptoms: Fever.
● Effectively treat Helicobacter
pylori infections by reducing LONG-TERM AND SERIOUS
stomach acid, which enhances ADVERSE EFFECTS
antibiotic efficacy and promotes 1. Gastric Cancer: Increased risk,
healing of the gastric lining. especially with prolonged use.
2. Bone Health: Long-term use can
Contraindications and Cautions lead to bone loss and increased
These drugs are contraindicated in the risk of fractures due to
presence of known allergy to either the decreased calcium absorption.
drug or the drug components to 3. Electrolyte Imbalances:
prevent hypersensitivity reactions, Decreased calcium and
They are also contraindicated to be magnesium levels, which can
used concurrently with medications contribute to hypertension and
containing rilpivirine. Caution should other complications.
be used in pregnant or lactating 4. Infections: Increased risk of
patients because of the potential for Clostridium difficile (C. difficile)
adverse effects on the fetus or neonate diarrhea and pneumonia due to
SIDE EFFECTS altered stomach acidity.
1. CNS Effects: Dizziness, 5. Nutrient Absorption Issues:
headache, fatigue (asthenia), Altered acidity can impact
vertigo, insomnia apathy, and absorption of key nutrients,
dream abnormalities. especially calcium and
2. Gastrointestinal Issues: magnesium.
Diarrhea, abdominal pain,
nausea, vomiting, dry mouth, INTERVENTION WITH RATIONALE
and tongue atrophy. 1. Administer the drug as
3. Respiratory Symptoms: Cough, prescribed. Ensure that the
stuffy nose, hoarseness, and patient does not open, chew, or
nosebleeds (epistaxis). crush capsules; they should be

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swallowed whole to ensure the II. GI PROTECTANTS
therapeutic effectiveness of the
drug. 1. Anatomy of the GI Tract

2. Provide appropriate safety and


The GI tract is a continuous tube extending
comfort measures if CNS effects from the mouth to the anus. It consists of the
occur to prevent patient injury. following main structures:

3. Monitor the patient for diarrhea


● Esophagus: A muscular tube that
or constipation to institute an connects the throat to the stomach,
appropriate bowel program as transporting food and liquids.
needed. ● Stomach: A muscular organ that
secretes digestive enzymes,
4. Monitor the patient's nutritional
hydrochloric acid (HCl), and mucus. It
status; if Gl upset is a problem,
plays a key role in breaking down food
the use of small, frequent meals and regulating the release of partially
may be helpful. digested food into the small intestine.

5. Arrange for medical follow-up if ● Small Intestine: Further digests food


and absorbs nutrients.
symptoms are not resolved after
● Large Intestine: Absorbs water and
4 to 8 weeks of therapy because forms waste for excretion.
serious underlying conditions
could be causing the symptoms. 2. Physiology of Gastric Acid Production

6. Offer support and The stomach lining has specialized cells that
encouragement to help the contribute to the digestion process, including:
patient cope with the disease
● Parietal Cells: These cells secrete
and the drug regimen.
hydrochloric acid (HCl), lowering
7. Provide thorough patient stomach pH and aiding in digestion.
teaching, including the drug HCl production is stimulated by signals

name and prescribed dosage, from histamine (via H2 receptors),


acetylcholine, and gastrin.
the importance of taking the
● Chief Cells: Produce pepsinogen, which
drug whole without opening, is activated by HCl to become pepsin, a
chewing, or crushing; signs and digestive enzyme that breaks down
symptoms of possible adverse proteins.
● Mucus Cells: Secrete mucus that lines
effects and measures to
the stomach walls, forming a protective
minimize or prevent them

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barrier against the harsh acidic areas, creating a physical
environment. barrier that protects these
● Prostaglandins: Compounds in the areas from stomach acid and
stomach that enhance blood flow, digestive enzymes.
promote mucus and bicarbonate ○ Misoprostol: This prostaglandin
secretion, and inhibit acid secretion, analog mimics the action of
thus protecting the stomach lining. natural prostaglandins,
promoting mucus and
MECHANISMS OF GI Protectant Drugs bicarbonate production and
enhancing mucosal blood flow,
GI protectants are used to reduce or neutralize
thus supporting the stomach’s
stomach acid, protect the mucosal lining, or
protective functions.
enhance mucus production to prevent or heal
● Bismuth Compounds: Bismuth
ulcers and other GI lesions. Here’s how each
subsalicylate provides a protective
class works within the anatomy and physiology
layer over ulcers and has mild
of the GI tract:
antimicrobial properties against H.
pylori, a bacterium linked to many
● Proton Pump Inhibitors (PPIs): These
peptic ulcers. This dual action helps in
drugs inhibit the H+/K+ ATPase enzyme
both protecting the lining and reducing
(proton pump) in the parietal cells of
ulcer-causing bacteria.
the stomach, reducing acid secretion.
By lowering acid levels, PPIs protect the
4. Physiological Responses to GI Protectants
stomach lining from erosion and
ulceration.
The body’s response to GI protectant drugs is
● H2 Receptor Antagonists: These drugs
primarily the preservation and restoration of
block the action of histamine on H2
the mucosal lining. By decreasing the
receptors in parietal cells, reducing the
production of acid or providing a protective
production of gastric acid. With lower
layer over the stomach lining, GI protectants
acid levels, the mucosa is less prone to
allow damaged tissues to heal while reducing
damage and irritation, promoting
the risk of further injury. The body relies on these
healing of ulcers.
drugs to counteract factors that may disrupt
● Antacids: Antacids neutralize excess
the protective mucus layer, allowing tissues to
stomach acid by increasing the pH in
repair without continued acid or pepsin
the stomach. They provide quick,
exposure.
symptomatic relief for acid-related
discomforts but do not reduce acid
Summary of GI Protectant Actions
production.
● Cytoprotective Agents:
● PPIs and H2 Antagonists lower
○ Sucralfate: When ingested,
acid production to reduce
sucralfate forms a gel-like layer
that adheres to ulcerated mucosal irritation.

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● Antacids neutralize acid, means less irritation to the
providing rapid relief. stomach lining.
● Cytoprotective Agents and 3. Proton Pump Inhibitors (PPIs):
Bismuth Compounds enhance Medications like omeprazole
mucosal protection by forming and pantoprazole inhibit the
physical barriers or increasing proton pumps in stomach cells,
protective secretions. which produce acid. They
reduce acid significantly,
Understanding the interplay of
helping prevent and heal ulcers.
stomach anatomy and acid secretion
4. Sucralfate: This forms a
physiology is fundamental to utilizing
protective coating over ulcers in
GI protectants effectively for treating
the stomach and intestines,
and preventing GI disorders such as
shielding them from acid, bile,
ulcers, gastritis, and GERD.
and enzymes. It doesn’t lower

MECHANISM OF ACTIONS acid but instead creates a

Gastrointestinal protectants help barrier.

shield the stomach and intestines from 5. A prostaglandin analog,

damage, often by forming a barrier or misoprostol mimics protective

reducing acid. stomach prostaglandins,


enhancing the mucus lining and

1. Antacids: These neutralize promoting bicarbonate

stomach acid, quickly reducing secretion, which buffers acid.

acidity to relieve symptoms like This is especially helpful for

heartburn. They don't affect acid people taking NSAIDs.

production but temporarily raise


the pH in the stomach. DRUGS UNDER CLASSIFICATION

2. H2 Receptor Antagonists: Drugs Proton Pump Inhibitors (PPIs)

like ranitidine and famotidine These drugs reduce gastric acid

block histamine (H2) receptors production by blocking the enzyme in

in the stomach lining, reducing the stomach lining responsible for acid

acid production. Less acid secretion.

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● Examples: Omeprazole, Bismuth Compounds
Esomeprazole, Pantoprazole, These help protect the stomach lining
Lansoprazole by forming a barrier over ulcers and
may also have mild antibacterial
H2 Receptor Antagonists
effects against Helicobacter pylori.
These drugs block histamine receptors
in the stomach, reducing acid ● Example: Bismuth subsalicylate
production. (Pepto-Bismol)

● Examples: Ranitidine, Prostaglandin Analogs


Famotidine, Cimetidine These help enhance mucus production
and increase blood flow to the
Antacids
stomach lining.
These drugs neutralize stomach acid
to relieve heartburn and indigestion. ● Example: Misoprostol (often
used in cases where
● Examples: Aluminum hydroxide,
NSAID-induced ulcers are a risk)
Magnesium hydroxide, Calcium
carbonate (Tums), Sodium
bicarbonate INDICATIONS
● Peptic Ulcer Disease (PUD)
Cytoprotective Agents
- GI protectants help in
These drugs protect the stomach lining
managing ulcers in the
by coating it, forming a protective
stomach or duodenum by
barrier, or stimulating mucus
creating a protective
production.
barrier and reducing acid

● Sucralfate: Forms a protective exposure.

coating over ulcers to shield


them from acid and pepsin. ● Gastroesophageal Reflux

● Misoprostol: A prostaglandin Disease (GERD)

analog that enhances mucus - These medications can

and bicarbonate secretion, reduce acid damage and

helping protect the stomach help manage the

lining. discomfort of acid reflux.

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protectants help in healing and
● NSAID-Induced Gastric Damage reducing further irritation.
- Long-term use of NSAIDs
(non-steroidal
anti-inflammatory drugs) can CONTRAINDICATIONS
lead to gastric ulcers. GI ● Renal Impairment: Avoid
protectants are used to prevent or adjust doses for
or heal this damage. antacids, H2 receptor
antagonists, and
● Stress Ulcers sucralfate.
- In critically ill patients, stress ● Pregnancy: Avoid
can lead to gastric mucosal misoprostol.
injury. Protectants are often ● Allergy: Be cautious with
given as a preventive measure. any hypersensitivity to
specific drug
● H. pylori Infection components.
-Some GI protectants, along ● Drug Interactions:
with antibiotics, help in the Consider potential
eradication of Helicobacter interactions, especially
pylori bacteria, which can cause with PPIs and H2 blockers.
ulcers.

● Zollinger-Ellison Syndrome SIDE EFFECTS


-This condition involves high
Common types of GI protectants
acid production, so GI
include proton pump inhibitors (PPIs),
protectants are used to control
H2 blockers, antacids, and sucralfate.
acid levels and prevent
While they are generally considered
damage.
safe, they can have side effects, which
vary depending on the specific type of
● Erosive Esophagitis
medication.
-when the esophagus lining is
damaged by stomach acid, GI

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Here are some possible side effects of ○ Rarely, changes in heart
common GI protectants: rate (bradycardia)
3. Antacids (e.g., calcium
1. Proton Pump Inhibitors (PPIs)
carbonate, magnesium
(e.g., omeprazole,
hydroxide):
lansoprazole):
○ Constipation (from
○ Headache
calcium or
○ Diarrhea or constipation
aluminum-based
○ Nausea or vomiting
antacids)
○ Abdominal pain or
○ Diarrhea (from
bloating
magnesium-based
○ Increased risk of
antacids)
infections (e.g.,
○ Electrolyte imbalances
Clostridium difficile,
(e.g., high calcium or
pneumonia) due to
magnesium levels)
reduced stomach acid
○ Stomach cramps
○ Long-term use may lead
○ Kidney stones (with
to nutrient deficiencies
excessive use)
(e.g., vitamin B12,
4. Sucralfate:
magnesium)
○ Constipation
○ Kidney disease (in rare
○ Nausea
cases)
○ Dry mouth
○ Bone fractures (with
○ Dizziness
long-term use)
○ Rash (rare)
2. H2 Blockers (e.g., ranitidine,
○ Can interfere with the
famotidine):
absorption of other
○ Headache
medications if taken at
○ Dizziness
the same time.
○ Constipation or diarrhea
○ Fatigue ADVERSE EFFECTS
○ Confusion (especially in 1. Sucralfate
elderly patients or those ★ Aluminum toxicity
with kidney issues) (especially in patients

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with kidney dysfunction, ★ Hepatotoxicity (potential
as sucralfate contains liver injury with long-term
aluminum) or high-dose use)
★ Hypophosphatemia (due ★ Arrhythmias (especially
to binding phosphate in when given intravenously
the gut) in high doses or in
★ Bezoar formation (rare patients with renal
but serious, involving a dysfunction)
solid mass in the ★ Pancytopenia or
digestive tract) neutropenia (rare cases
2. Proton Pump Inhibitors (PPIs) of blood dyscrasias)
★ Increased risk of bone ★ Central nervous system
fractures (due to possible effects (especially in the
calcium malabsorption elderly, causing
with long-term use) confusion, hallucinations,
★ Clostridioides difficile (C. or seizures)
difficile) infection 4. Antacids
(increased risk due to ★ Hypermagnesemia
reduced stomach acidity, (excessive magnesium
which affects gut flora can cause serious issues
balance) such as weakness, low
★ Kidney disease or acute blood pressure, and even
interstitial nephritis cardiac arrest, especially
★ Increased risk of gastric in patients with kidney
cancer (associated with dysfunction.
prolonged use) ★ Hypophosphatemia
★ Vitamin and mineral (aluminum can bind
deficiencies (particularly phosphate in the gut,
B12, iron, and magnesium, leading to low phosphate
potentially leading to levels, which can cause
neurological or muscular muscle weakness and
symptoms) bone pain).
3. H2-Receptor Antagonists

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★ Hypercalcemia (elevated other medications requiring
calcium levels can lead to acidic pH.
kidney stones, impaired ● Sucralfate: This can reduce the
kidney function, and absorption of drugs like digoxin,
metabolic alkalosis). warfarin, phenytoin, and
tetracycline by forming
INTERACTIONS complexes with them, thus
decreasing their bioavailability.
● Clopidogrel: PPIs like
omeprazole may reduce the NURSING MANAGEMENT
effectiveness of clopidogrel. This Assessment
can increase the risk of
cardiovascular events. 1. Assess for Abdominal Pain:
● Warfarin: PPIs may increase the Assess for the location, intensity,
anticoagulant effect of warfarin, and duration of pain, especially
raising the risk of bleeding. epigastric pain or heartburn.
● Digoxin: PPIs can increase the This helps evaluate the
absorption of digoxin, leading to effectiveness of the GI
potential toxicity. protectant.
● Ketoconazole/Itraconazole: PPIs 2. Assess for Bowel Pattern: Monitor
can reduce the absorption of for constipation or diarrhea,
these antifungal drugs, which common side effects of some GI
require an acidic environment protectants (e.g., sucralfate can
for optimal absorption. cause constipation, while
● Methotrexate: High-dose magnesium-containing
methotrexate therapy may antacids may cause diarrhea).
interact with PPIs, increasing 3. Stool Observation: Look for black,
methotrexate toxicity. tarry stools, which can be a sign
● Antacids: When antacids are of GI bleeding, especially in
used concurrently with H2 patients with a history of ulcers.
blockers, they may reduce the 4. Assess for the Symptoms:
absorption of H2 blockers or Assess if GI symptoms like
heartburn, acid reflux, or

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epigastric pain are improving, 2. Assess the intensity and
which indicates that the frequency of headaches. If
medication is working as needed, consult the provider for
intended. analgesic medication that does
5. Assess for Neurological Effects: not interfere with its action.
Some GI protectants, like 3. Educate the patient on infection
aluminum-based antacids or prevention practices, such as
bismuth subsalicylate, can regular handwashing and
cause dizziness, confusion, or reporting any signs of
headache, especially in older gastrointestinal infections
adults. promptly.
4. Assess for fatigue patterns.
Nursing Diagnosis Encourage rest and assist with
daily activities if needed.
Constipation due to the use of GI 5. Encourage small, frequent
protectant drugs as evidenced by meals and advise against
abdominal discomfort, decreased high-fat or gas-producing
frequency of bowel movements, and foods.
difficulty passing tool 6. Offer small sips of water and
provide sugar-free lozenges or
P (Problem): Constipation ice chips to manage dry mouth.
E (Etiology): Related to the use of Administer sucralfate on an
GI-protectant drugs empty stomach to minimize
S (Signs/Symptoms: Evidenced by nausea.
abdominal discomfort, decreased 7. Instruct patients to report any
frequency of bowel movements, and onset of diarrhea, abdominal
difficulty passing tool cramping, and fever
Nursing Intervention 8. Observe patients for signs of
arrhythmias, particularly if they
1. Monitor bowel patterns and have renal dysfunction or are on
encourage fluid intake if there is intravenous high-dose therapy,
a presence of dehydration if monitoring for palpitations,
diarrhea occurs. dizziness, or irregular heartbeat.

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9. Encourage patients to stay Nerves
hydrated, maintain a balanced ● The enteric nervous system,
diet, and report any unusual which is located in the wall of
symptoms promptly. the gut, controls Gl motility.
10. Screen patients on long-term Enteric neurons release
PPIs for signs of bone density neurotransmitters like
loss, particularly older adults acetylcholine, serotonin, and
who may be at higher risk for cholecystokinin to regulate
fractures. bowel motility.
Hormones
● Peptides like gastrin and motilin
III. Drugs Affecting GASTROINTESTINAL
are released into the blood after
MOTILITY
eating. and act as hormones to
Gastrointestinal Motility activate the gut.
- Is the process by which the
digestive tract moves food and ● Drugs affecting Gl motility are
mixes it with digestive enzymes classified based on their effects
for digestion and absorption. It on the smooth muscle of the Gl
involves the coordination of the tract, often targeting disorders
muscular layers of the GI tract. like constipation, diarrhea, or
Called the tunica muscularis, conditions causing abnormal
with nerves and hormones motility such as irritable bowel
syndrome (IBS).
Smooth Muscle
● The muscular layers of the GI Review of GI Anatomy and Physiology
tract are made up of smooth Related to Motility
muscle cells that are organized Anatomy
into circular and longitudinal • The Gl tract includes the esophagus,
bundles. These cells are stomach, small intestine, and large
electrically and mechanically intestine, surrounded by smooth
connected, which allows them muscle layers responsible for motility.
to contract in a coordinated
way.

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• Myenteric Plexus: Regulates • Serotonin Agonists: Promote
peristalsis and coordinated serotonin receptor activity to enhance
contractions. motility.
• Submucosal Plexus: Controls 2. Antispasmodics
secretions and blood flow. (Spasmolytics)
Physiology These drugs reduce smooth muscle
• Peristalsis: Wave-like contractions contraction, relieving spasms and
that propel food forward. pain.
• Segmentation: Localized contractions Mebeverine:
for mixing and digestion. • Directly acts on Gl smooth muscle to
• Controlled by the enteric nervous reduce spasm without affecting
system, influenced by.: autonomic normal motility.
inputs and local hormones like Peppermint oil:
serotonin; motilin, and gastrin. • Acts as a calcium channel antagonist
on smooth muscle to relax spasms.
MECHANISM OF ACTIONS
1. Prokinetic Agents 3. Laxatives
- Drugs that help improve the - increase bowel movements
movemement of the digestive different mechanisms to treat
system constipation. By
•Target smooth muscle and enteric Bulk-forming laxatives (e.g.,
nervous system. Psyllium, Methy|cellulose):
• Enhance neurotransmitter activity ● Increase stool bulk by absorbing
(e.g., acetylcholine) or receptor water, stimulating intestinal
interactions. motility.
Osmotic laxatives (e.g., Lactulose,
Key pathways:
Polyethylene glycol, Magnesium
•Cholinergic Agonists: Stimulate
salts):
acetylcholine release.
● Draw water into the intestine,
•Dopamine Antagonists: Block inhibitory
softening stools and increasing
dopamine effects on GI motility.
peristalsis.

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- Drink plenty of water to avoid to produce a bowel
blockages. movement.
Drug Class: Laxative: Stimulant
Serotonergic Modulators Pharmacokinetics:
Drugs that target serotonin receptors ● Absorption: minimal (5-15%)
to modulate motility. ● Distribution PB: UK
Tegaserod (5-HT4 agonist): ● MetabolismL t1/2: UK
● Promotes motility in conditions ● Excretion: in bile and urin
like irritable bowel syndrome
(IBS) with constipation.
Contraindication • Hypersensitivity
Alosetron (5-HT3 antagonist): s • Fecal impaction
● Reduces motility and secretions, • Intestinal/biliary
used in IBS with diarrhea. obstruction
• Gl Bleeding
• Appendicitis
LAXATIVES
• Abdominal Pain
Laxatives and cathartics are used to
• Nausea
eliminate fecal matter. Laxatives • Vomiting
promote a soft stool, cathartics result
in a soft to watery stool with some Cautions • Diarrhea
• Diverticulitis
cramping, and frequently dosage
• Electrolyte
determines whether a drug acts as a
Imbalance
laxative or cathartic. • Ulcerative
1. Bisacodyl Colitis
- A laxative that comes in
tablet or capsule form to SIDE EFFECTS
treat occasional • Dependence
constipation. • Hypokalemia
- Constipation occurs when ADVERSE EFFECTS
you have less frequent • Dizziness
bowel movements. This • Anorexia
medication works by • Nausea
helping the muscles in • Vomiting
your intestines move stool

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• Abdominal Cramps • Excretion: Psyllium is fermented
• Diarrhea partially by gut bacteria, and the rest is
• Rectal Burning excreted in feces.

INTERACTIONS INDICATION
• Drug • Primary: Relief of constipation.
● Decreased effect with antacids, • Secondary:
histamine 2 blockers, proton • Management of irritable bowel
pump inhibitors syndrome (IBS).
Food • Regulation of stool in diarrhea or
• Milk loose stools.
• Adjunctive therapy for hyperlipidemia
BULK-FORMING LAXATIVE (helps reduce cholesterol levels by
● They mimic dietary fiber and are binding bile acids in the gut).
often recommended as a • Control of blood sugar levels in
first-line treatment for mild or diabetes mellitus by slowing glucose
chronic constipation. absorption.
● Psyllium is a bulk-forming
laxative derived from the seeds
of the Plantago ovata plant. It is • Known
widely used to manage hypersensitivity to
constipation and other the product.
gastrointestinal conditions by • Bowel obstruction
increasing stool bulk and or suspected
CONTRAINDICATION intestinal blockage.
improving bowel movements.
• Fecal impaction.
PHARMACOKINETICS
• Difficulty
• Absorption: Not systemically
swallowing or risk
absorbed; acts locally in the
of choking.
gastrointestinal tract.
• Severe
• Onset of Action: Usually takes 12-72 dehydration or
hours for effects to manifest. electrolyte
imbalance.

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1.Assess baseline bowel patterns
• Esophageal or
(frequency, consistency, ease of
intestinal
defecation).
• Bloating.
2. Evaluate for contraindications like
obstruction if
bowel obstruction, fecal impaction, or
taken without
swallowing difficulties
SIDE EFFECTS • Gas
(flatulence).
OSMOTIC LAXATIVES
sufficient water.
● Are medications that have
• Mild abdominal
solutes that increase osmotic
cramping.
pull of fluid into the Gl tract. This
will increase pressure in the Gl
ADVERSE EFFECT
tract and stimulate more
• Esophageal or intestinal
intestinal motility.
• Bloating.
MAGNESIUM CITRATE
obstruction if taken without
● Magnesium citrate works by
• Gas (flatulence). sufficient water.
saline pull, bringing fluids into
• Mild abdominal cramping.
the lumen of the GI tract. This
• Rare allergic reactions (e.g.,
product is used to clean stool
rash, itching, difficulty breathing).
from the intestines before
• Severe abdominal pain or persistent
surgery or certain bowel
bloating (rare, but may indicate
procedures, it is also used to
obstruction).
relieve constipations.
• Decreased Drug Absorption: Psyllium
PHARMACOKINETICS
can interfere with the absorption of:
● Onset of 30 minutes to 4 hours
• Digoxin, warfarin, and salicylates.
absorption varies with type of
• Separate administration by at least 2
magnesium substance, highly
hours.
bound to plasma proteins,
• Hypoglycemics: May enhance blood
excreted kidneys.
sugar control; dose adjustments of
CONTRAINDICATION & CAUTIONS
antidiabetic medications might be
● LAXATIVES are contraindicated
necessary.
in patients with acute surgical
NURSING INTERVENTION

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abdomen, fecal impaction, or ● Mostly associate with this drug
intestinal obstruction. Lactulose are primarily related to its GI
is a disaccharide and so should effects.
be used with caution in patients ● These effects may be related to
with diabetes. a sympathetic stress reactions
ADVERSE EFFECTS to intense neurostimulation of
● Most commonly associated with the Gl tract or the loss of fluid.
osmotic laxative are Gl effects CONTRAINDICATION & CAUTIONS
(diarrhea, abdominal cramps, ● Same with Magnesium citrate, it
bloating) and symptoms of is also contraindicated with
dehydration. acute sugical abdomen.
● CNS effects (dizziness, ● Polyethylene glycol electrolyte
headache and weakness, are solution should be used with
not uncommon and may relate caution in any patient with
to loss of fluid. history of seizures because at
● electrolyte imbalances that may risk of electrolyte wasting
accompany laxative use. causing neuronal instability.
NURSING CONSIDERATIONS ANTI-DIARRHEAL DRUGS
• Asses for possible contraindication of LOPERAMIDE (IMODIUM)
cautions: any history of allergy to SIDE EFFECT
Magnesium citrate to prevent • Constipation
hypersensitivity reaction; fecal • Abdominal Discomfort
impaction or intestinal obstruction. • Dry Mouth
• Perform a physical examination to • Nausea and Vomiting
establish baseline data before • Dizziness
beginning of theraphy. • Fatigue
• Assess patient's neurological status, ADVERSE EFFECT
including level of orientation affect, • Toxic Megacolon
and reflexes, to monitor for CNS effect • Heart Problems (Cardiac Effects)
of the drug. • Respiratory Depression
• Central Nervous System Effects (in
OSMOTIC LAXATIVE Overdose)
ADVERSE EFFECT

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• Severe Allergic Reactions ● Excreted mainly in urine, with
(Anaphylaxis) some fecal elimination. With a
• Pseudomembranous Colitis (in Cases half-life of 2-3 hours, but effects
of may last longer due to its action
Overuse or Misuse) on the Gl tract.
DRUG INTERACTION INDICATION
● interacts with drugs that inhibit • Acute Diarrhea: For symptomatic
CYP3A4 or P-glycoprotein, relief of acute diarrhea in adults and
increasing the risk of toxicity children (over 2 years).
(e.g., cardiac arrhythmias, CNS • Chronic Diarrhea: May be used for
depression). It may be less chronic functional diarrhea, though it's
effective when used with not first-line.
CYP3A4 inducers. CONTRAINDICATION
NURSING INTERVENTION • Hypersensitivity: Known allergy to
● Monitor hydration status, check diphenoxylate or atropine.
for contraindications, and • Infectious Diarrhea: Should not be
educate patients about proper used for diarrhea caused by bacterial
use and the risks of misuse, infections (e.g.,
overdose, and adverse effects. Salmonella, Shigella, C. difficile).
• Pseudomembranous Colitis:
DIPHENOXYLATE Contraindicated in patients with this

● helps the body absorb more condition.

water from the stool, resulting in • Children under 2 years: Risk of

firmer stools and less frequent respiratory depression.

bowel movements. • Obstructive Jaundice:

PHARMACOKINETICS Contraindicated in patients with liver

● Absorbed from the Gl tract. disease or biliary obstruction.

Primarily metabolized by the SIDE EFFECT

liver via CYP3A4 and CYP2C8 • Drowsiness

enzymes to its active • Dry mouth (due to atropine)

metabolite, diphenoxylic acid. • Constipation


• Abdominal discomfort or bloating
• Nausea or vomiting

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ADVERSE EFFECT NURSING INTERVENTION
• Respiratory depression (particularly • Monitor hydration, bowel movements,
with overdose or misuse) and vital signs (especially respiratory
• Tachycardia and other and cardiovascular status).
cardiovascular effects (due to • Educate the patient on the proper use
atropine) of the medication, potential side
• Dependence or abuse potential, effects, and the importance of
especially in patients with opioid use hydration.
history • Be cautious with vulnerable
• Toxic megacolon populations (elderly, children,
in patients with pregnant women).
inflammatory bowel disease (IBD) • Monitor for adverse effects,
DRUG INTERACTION particularly respiratory depression and
• CNS Depressants: Enhanced CNS cardiovascular changes.
depression and risk of respiratory
failure. OPIOID ANTAGONISTS
• MAO Inhibitors: Increased NALOXEGOL(MOVANTIK)
anticholinergic effects and risk of Indication:
hypertensive crises. • Used to treat opioid-induced
• Anticholinergic Drugs: Worsened constipation (OIC) in adults with
side effects like dry mouth, chronic non-cancer pain
constipation, and blurred vision. Contraindications:
• CYP3A4 Inhibitors: Increased • Known or suspected gastrointestinal
diphenoxylate levels and risk of (Gl) obstruction
adverse effects. • Severe hypersensitivity to naloxegol
• CYP3A4 Inducers: Reduced or any component of the formulation
effectiveness of diphenoxylate. • Concurrent use with strong CYP3A4
• QT-Prolonging Drugs: Increased risk inhibitors.
of arrhythmias.
• Opioids: Potential for compounded
side effects, including respiratory
depression and constipation.

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Side Effects:
Nursing Interventions:
Nausea,
• Assess the patient's baseline bowel
vomiting,
Common habits, including frequency and
abdominal pain,
consistency of stools.
diarrhea, gas,
• Review the patient's current opioid
headache
regimen and any history of
Severe or opioid-induced constipation.
worsening • Perform a thorough medical history,
abdominal pain, including any known gastrointestinal
diarrhea, opioid obstructions.
withdrawal • Monitor for signs of opioid withdrawal,
Serious
symptoms including increased pain, sweating,
(anxiety,irritability anxiety, and irritability.
,sweating,chills, • Assess the patient's bowel
yawning, movements regularly to evaluate the
stomach pain, effectiveness of the medication.
diarrhea) • Monitor for signs of severe or
persistent abdominal pain, which

Adverse Effects: could indicate a serious condition such

• Severe Gl perforation as gastrointestinal perforation.

• Increased risk of recurrent Gl


obstruction METHYLNALTREXONE

Interactions: BROMIDE (RELISTOR)

• Strong CYP3A4 inhibitors (e.g., Contraindications:

atazanavir, clarithromycin) can • Used to treat opioid-induced

significantly increase naloxegol levels, constipation (OIC) in patients with

potentially causing opioid withdrawal chronic non-cancer pain who have not

symptoms responded adequately to laxatives

• Strong CYP3A4 inducers (e.g., • Known or suspected obstruction

carbamazepine) are not • Severe hypersensitivity

recommended methylnaltrexone
or component of the formulation

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LUBRICANT (2) DOCUSATE SODIUM (STOOL


GLYCERIN SUPPOSITORIES SOFTENER)
It works by helping the stool absorb
SIDE EFFECT water, making it softer and easier to
• Rectal Irritation or Discomfort pass. Unlike stimulant laxatives, which
• Abdominal Cramping or Bloating induce bowel movements by
• Diarrhea stimulating the muscles of the
• Nausea intestine, docusate sodium is a mild,
ADVERSE EFFECT non-irritating laxative that is generally
• Severe Rectal Irritation or Injury well tolerated for long-term use in
• Electrolyte Imbalance most individuals.
• Severe Abdominal Pain or Distension
• Risk of Dependence PHARMACOKINETICS
• Allergic Reactions The extent to which orally administered
DRUG INTERACTION docusate salts are absorbed has not
● Glycerin suppositories are been determined, but the drugs
primarily locally acting and are appear to be absorbed to some extent
not significantly absorbed into in the duodenum and jejunum and
systemic circulation. Because of subsequently excreted in bile. The
this, the potential for drug extent of absorption following rectal
interactions is minimal. While administration of docusate sodium is
glycerin suppositories are unknown.
generally low-risk for drug
interactions, caution should be INDICATION
taken when used with • It is used for the short-term relief of
medications that can constipation, especially in individuals
NURSING INTERVENTION who should avoid straining (e.g.,
Ensure that glycerin suppositories are post-surgery, hemorrhoid patients,
administered safely, effectively, and and individuals with cardiovascular
with minimal adverse effects, while problems).
also supporting the patient's overall • It is often recommended for patients
gastrointestinal health. who need to soften their stool for

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medical reasons, such as after ● docusate sodium generally has
childbirth or abdominal surgery. a low risk for drug interactions, it
is still important to monitor for
CONTRAINDICATION potential interactions with other
• Avoid overuse, as excessive use can laxatives, diuretics,
lead to electrolyte imbalances or anticoagulants, and
dependency on laxatives. medications that affect
• Contraindicated in patients with electrolytes. Caution should be
intestinal obstruction or acute exercised in patients using
abdominal pain (as it could worsen multiple medications that can
these conditions). affect hydration or electrolyte
• Use with caution in individuals with balance.
renal impairment due to potential
changes in fluid balance. IRRITABLE BOWEL
SYNDROME AND CHRONIC
SIDE EFFECT CONSTIPATION DRUGS
• Mild abdominal cramping ● IBS is a common disorder. It
• Diarrhea (if overused) affects three times as many
• Nausea or a bitter taste (in some oral females as males and
formulations) reportedly accounts for half oF
• Fatigue all referrals to Gl specialists.
• Muscle weakness ● The disorder is characterized by
• Cramping abdominal distress, bouts of
diarrhea or constipation,
ADVERSE EFFECT bloating, nausea, flatulence,
• Abdominal Cramping headache, fatigue, depression
• Diarrhea and anxiety has been found for
• Nausea this disorder.
• Bloating ● Underlying causes might be
• Rectal Discomfort stress and/or dysregulation of
the autonomic nervous system.
DRUG INTERACTION ● Patients with this disorder have
often suffered for years, not

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enjoying meals or activities • Chronic or severe constipation or
because of their Cl pain and sequelae
discomfort. from constipation
ALOSETRON • Intestinal Obstruction
LOTRONEX • Stricture
USUAL DOSAGE • Toxic megacolon
● Adult Female: 0.5mg PO BID as • GI perforation and/or lesions
initial dose: May be increased to
1mg PO BID after 4 weeks if well CAUTION
tolorated • Alosetron may cause serious
USUAL INDICATIONS gastrointestinal (GI;
● Treatment of severe affecting the stomach or intestines)
diarrhea-predominant IBS: - in side effects including ischemic colitis
patients who have chronic IBS (decreased blood flow to the bowels)
symptoms (generally lasting 6 and severe constipation that may
mo or longer), had anatomic or need to be treated in a hospital and
biochemical abnormalities of may rarely cause death.
the gastrointestinal tract
excluded, and did not respond PHARMACOKINETIC
adequately to conventional ROUTE: ORAL
therapy ONSET: UNKNOWN
MECHANISM OF ACTION PEAK: 60 MINUTES
SELECTIVE 5-HT3 RECEPTOR DURATION: UNKNOWN
ANTAGONIST FOR RECEPTORS IN THE GI
TRACT. BY BLOCKING THESE RECEPTORS, Half life: 1.5 hours; metabolized in the
THE MEDICATION IS ABLE TO MODULATE liver and excreted via the kidneys.
PAIN AND SLOW MOTILITY AND GI
SECRETIONS SIDE EFFECTS
• upset stomach
• nausea
CONTRAINDICATION • gas
• swelling in the stomach area
• hemorrhoids

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• Provide thorough patient teaching,
ADVERSE EFFECT including the drug name and
• Constipation prescribed dosage, measures to help
• Abdominal avoid adverse effects, warning signs
Discomfort and Pain that may indicate problems, and the
• Nausea need for periodic monitoring and
• Ischemic Colitis evaluation, to enhance, patient
knowledge about drug therapy and to
DRUG INTERACTION promote adherence.
• Medications that slow GI motility can
increase risk of constipation if taken
concurrently with Alosetron or
Eluxadoline. Concurrent use of
Alosetron and CYP1A2 inhibitors can
increase exposure to Alosetron; use
with fluvoxamine is contraindicated.

NURSING CONSIDERATION &


INTERVENTION
• Assess for possible contraindications
or cautions: any history of allergy to
these drugs to prevent hypersensitivity
reactions; intestinal obstruction,
bleeding, or perforation, which could
be exacerbated by stimulating the GI
tract; and current status of pregnancy
or lactation, which require cautious
use.
• Offer support and encouragement to
help the patient deal with the
diagnosis and the drug regimen,
including the abdominal discomfort
and altered Gl motility.

50

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