PHARMACOLOGY

FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

5. AGGREGATION
platelets clump to form plug & stop bleeding
Finals Topic:
- Drugs Affecting Blood Coagulation
- Dosage and Calculations
- Lipid Lowering Agents
- GIT Drugs
- ANS Drugs
- Cardiac Drugs

DRUGS AFFECTING BLOOD COAGULATION

BLOOD COAGULATION
- also known as clotting, is the process by which blood
changes from a liquid to a gel, forming a blood clot.

INTRINSIC VS EXTRINSIC PATHWAY

refers to the multiple refers to multiple cascades
cascades of protein of protein interactions
interactions activated by activated by damaged
trauma inside blood vessels external surfaces
CLOTTING PROCESS
1. Damaged vessel endothelium is a stimulus to activated by internal trauma activated by external trauma
circulating platelets, causing platelet adhesion.
2. Platelets release mediators, and platelet aggregation factors VIII, IX, XI, and XII factor VII is involved
results are involved

Platelet Plug Formation slow fast

PRIMARY HEMOSTASIS
1. INJURY 15-20s for the initiation of 2-6mins. for the initiation of
endothelial cells secrete endothelin blood clotting blood clotting
→ narrow blood vessel, decrease blood loss
requires ionized calcium for required both calcium and
the activation of factor IX by tissue factor for the
2. EXPOSURE
factor IXa activation of factor IX by
endothelial cells release von willebrand's factor
factor VIIa
→ binds to exposed collagen

3. ADHESION VITAMIN K DEPENDENT CLOTTING

platelets bind to von willebrand factor FACTORS
1972
4. ACTIVATION ● Factor X – Stuart
platelets activate & release von willebrand factor, serotonin, ● Factor IX – Christmas
ADP, & thromboxane a2 to attract & activate more platelets ● Factor VII – Stable
● Factor II - Prothrombin

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PHARMACOLOGY
FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

CLOT RESOLUTION - treat CV diseases that are prone to produce occluded

A. Anticlotting process vessels
- Antithrombin III (in plasma) and rivaroxaban inhibit the - maintenance of venous and arterial grafts
activity of Stuart factor (factor Xa) and thrombin - prevent cerebrovascular occlusion
- Heparin enhances the activity of antithrombin III. - as adjuncts to thrombolytic therapy in the treatment of
- Dabigatran directly inhibits thrombin myocardial infarction (MI)
- prevention of reinfarction after MI.
B. Fibrinolytic Process
- Clots are dissolved PHARMACOKINETICS
- are administered orally EXCEPT Abciximab,
PLASMIN OR FIBRINOLYSIN - dissolves clots to ensure free eptifibatide, and tirofiban which are thru intravenously
movement of blood through the system (IV)
- Dipyridamole is used orally or as an IV agent.
- well absorbed and highly bound to plasma proteins.
DISORDERS AFFECTING BLOOD COAGULATION
- metabolized in the liver
A. THROMBOEMBOLIC - excreted in the urine
★ Formation of thrombi result in decreased - can enter breast milk
blood flow through or total occlusion of a
blood vessel CONTRAINDICATIONS
★ S/Sx: hypoxia, anoxia, or even necrosis in - allergy
areas affected by the decreased blood flow. - pregnancy
★ Coronary Artery Disease - during lactation

B. HEMORRHAGIC CAUTIONS
★ Excess bleeding occurs - presence of any known bleeding disorder or active
★ Hemophilia bleeding
★ Liver Disease - recent surgery and closed head injuries
★ Bone Marrow Disorders - history of stroke, or transient ischemic attack (TIA)
- Anagrelide: with any history of thrombocytopenia
- Clopidogrel: for people who poorly metabolize a
DRUGS AFFECTING CLOT FORMATION AND
certain liver enzyme (CYP2C19)
RESOLUTION
ADVERSE EFFECTS
CNS
ANTIPLATELET AGENTS
- dizziness
- alter platelet aggregation and the formation of the GENERAL
platelet plug - increased bleeding
DRUGS IN FOCUS DERMATOLOGICAL
1. Abciximab - alopecia
2. Anagrelide - dermatitis
3. Aspirin OTHER
4. Cilostazol - bone marrow suppression
5. Clopidogrel
6. Dipyridamole
ASPIRIN
7. Eptifibatide
8. Prasugrel ➢ inhibits platelet aggregation by inhibiting platelet
9. Ticagrelor synthesis of thromboxane A2
10. Ticlopidine
11. Tirofiban INDICATIONS
12. Vorapaxar ● reduction of risk of recurrent TIAs or strokes in men
with a history of TIA due to fibrin or platelet emboli
INDICATIONS

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PHARMACOLOGY
FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

● reduction of death or nonfatal MI in patients with a - to enhance patient knowledge

history of infarction or unstable angina about drug therapy and to promote
● MI prophylaxis compliance with the drug regimen.
● antiinflammatory, analgesic, and antipyretic effects
TEST MEASURE THERAPEU USES
PHARMACOKINETICS TIC RANGE
- Route: Oral
- Onset: 5-30min aPPT Activity of 1.5-2.5 Dose adjustment
- Peak: 0.25-2hrs PTT intrinsic times for heparin,
- Duration: 3-6hr pathway of baseline low-molecular-weig
coagulation ht heparins,
T1/2 desirudin,
argatroban,
- 15 minutes to 12 hours, metabolized in the liver and
bivalirubin,
excreted in the urine dabigratan,
rivaroxaban
ADVERSE EFFECTS
- Acute aspirin toxicity with hyperpnea → leading to INR Standardized 2-3.5 Warfarin dose
fever, coma, and CV collapse measure of adjustment,
prothrombin fondaparinux dose
- nausea, dyspepsia, heartburn,epigastric discomfort,
levels adjustments
GI bleeding, occult blood loss, dizziness, tinnitus,
difficulty hearing, and anaphylactoid reaction. Time required 1.3-1.5 Warfarin dose
PT
for clotting to adjustment
NURSING CONSIDERATIONS occur; extrinsic
IMPLEMENTATION pathway activity
1. Provide small, frequent meals - relieve GI discomfort
if GI upset is a problem.
2. Provide comfort measures and analgesia for ANTICOAGULANTS
headache - relieve pain and improve patient
➢ interfere with the normal coagulation process by
compliance with the drug regimen.
interfering with the clotting cascade and thrombin
3. Suggest safety measures (use of an electric razor and
formation
avoidance of contact sports) - to decrease the risk of
bleeding
DRUGS IN FOCUS
4. Monitor platelet count if the patient is using
1. Antithrombin
anagrelide - to detect thrombocytopenia and
2. Apixaban
increased risk of bleeding
3. Argatroban
5. Provide increased precautions against bleeding
4. Betrixaban
during invasive procedures; use pressure dressings
5. Bivalirudin
and ice - to decrease excessive blood loss caused by
6. Dabigatran
anticoagulation.
7. Desirudin
6. Mark the chart of any patient receiving this drug - to
8. Edoxaban
alert medical staff that there is a potential for
9. Fondaparinux
increased bleeding.
10. Heparin
7. Offer support and encouragement - to help the patient
11. Protein C
deal with the diagnosis and the drug regimen
12. Concentrate
8. Provide thorough patient teaching:
13. Rivaroxaban
- name of the drug, dosage prescribed
14. Warfarin
- measures to avoid adverse effects
- warning signs of problems
- the need for periodic monitoring and WARFARIN
evaluation
- an oral drug
- the need to wear or carry a MedicAlert
notification

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

- causes a decrease in the production of vitamin - factor Xa inhibitors that stop the coagulation
K–dependent clotting factors in the liver à depletion of cascade
clotting factors and an extension of clotting times - for prevention of DVT (which might lead to
- Adverse Effects: Bleeding, alopecia, dermatitis, bone PE), in patients undergoing knee or hip
marrow suppression replacement surgery
- for prevention of stroke in patients with
nonvalvular AF
DRUG TO DRUG INTERACTIONS WITH WARFARIN - for the prevention and treatment of DVT and
PE
1. Increase Bleeding Effects
c. APIXABAN
Salicylates Oxyphenbutazone Thyroid
- factor Xa inhibitor
Chloral hydrate drugs
- caution: renal impairment
Phenylbutazone Clofibrate Glucagon
- approved for the treatment on nonvalvular
Disulfiram Chloramphenicol Danazol
AF and the treatment of DVT and PE
Metronidazole Erythromycin
Cimetidine Androgens
DRUG TO DRUG INTERACTIONS WITH NEW ORAL
Ranitidine Amiodarone Cefamandole
ANTICOAGULANTS
Cotrimoxazole Cefotetan
1. ALTERS METABOLISM of Dabigatran, Apixaban,
Quinidine Moxalactam
Rivaroxaban, Edoxaban
Quinine Cefazoline
- Antifungals
Meclofenamate Mefenamic Cefoxitin
- Erythromycin
Acid Nizatidine Ceftriaxone
- Ritonavir
Famotidine
- Phenytoin
Nalidixic Acid
- Rifampin
2. Cause HIGHER PLASMA LEVELS of Betrixaban
2. Decrease Anticoagulation - Amiodarone
- Azithromycin
Barbiturates Vitamin K
- Verapamil
Griseofulvin Vitamin E
- Ketoconazole
Rifampin Cholestyramine
- Clarithromycin
Phenytoin Aminoglutethimide
Glutethimide Ethchlorvynol
PHARMACOKINETICS
Carbamazepine

3. Incraese Activity And Effects Of Other Drug

- Phenytoin

NEWER ORAL DRUGS

a. DABIGATRAN
- directly inhibits thrombin
- approved to reduce the risk of stroke and
systemic embolism in patients with ➢ HEPARIN, ARGATROBAN, AND BIVALIRUDIN
nonvalvular atrial fibrillation - block the formation of thrombin from
- treatment of deep vein thrombosis (DVT) prothrombin
and pulmonary embolism (PE) in patients - given via IV
treated with a parenteral anticoagulant for 5 - excreted via urine
to 10 days
- prevention of recurrence of DVT and PE ➢ ANTITHROMBIN AND PROTEIN C CONCENTRATE
- replacement in specific genetic deficiencies
b. RIVAROXABAN AND EDOXABAN

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

- exogenous forms of naturally occurring - metabolized in the cells

anticoagulants - excreted in the urine

➢ ANTITHROMBIN ADVERSE EFFECTS

- interferes with the formation of thrombin from - Loss of hair, bruising, chills, fever, osteoporosis, and
prothrombin suppression of renal function
- a naturally occurring anticoagulant

➢ FONDAPARINUX NURSING CONSIDERATION

- inhibits factor Xa IMPLEMENTATION
- blocks the clotting cascade to prevent clot 1. Evaluate for therapeutic effects of warfarin—PT of 1.5
formation to 2.5 times the control value or ratio of PT to INR of 2
- given via SQ to 3 - to evaluate the effectiveness of the drug dose
- metabolized and excreted by the kidneys 2. Evaluate for therapeutic effects of
heparin—whole-blood clotting time (WBCT) of 2.5 to 3
CONTRAINDICATIONS times control or activated partial thromboplastin time
- presence of allergy (APTT) of 1.5 to 3 times the control value - to
- pregnancy & lactation: oral anticoagulants evaluate the effectiveness of the drug dose.
- hemorrhagic disorders, recent trauma, spinal 3. Evaluate the patient regularly for any sign of blood
puncture, GI ulcers, recent surgery, intrauterine loss (petechiae, bleeding gums, bruises, dark-colored
device placement, tuberculosis, presence of stools, darkcolored urine) - to evaluate the
indwelling catheters, and threatened abortion effectiveness of the drug dose and to determine the
- renal or hepatic disease need to consult with the prescriber if bleeding
becomes apparent.
CAUTIONS 4. Establish safety precautions - to protect the patient
- heart failure, thyrotoxicosis, senility or psychosis, from injury.
diarrhea or fever 5. Suggest safety measures (use of an electric razor and
avoidance of contact sports) - to decrease the risk of
bleeding
HEPARIN
6. Provide increased precautions against bleeding
- inhibits thrombus and clot production by blocking the during invasive procedures; use pressure dressings
conversion of prothrombin to thrombin and fibrinogen and ice; avoid IM injections; and do not rub
to fibrin subcutaneous injection sites - to decrease excessive
- does not enter breast milk blood loss caused by anticoagulation.
7. Mark the chart of any patient receiving this drug - to
USED FOR alert medical staff that there is a potential for
- acute treatment and prevention of venous thrombosis increased bleeding.
and PE 8. Offer support and encouragement - to help the patient
- treatment of AF with embolization - prevention of deal with the diagnosis and the drug regimen
clotting in blood samples and in dialysis and venous 9. Maintain antidotes on standby (protamine sulfate for
tubing heparin, vitamin K or prothrombin complex
- diagnosis and treatment of disseminated intravascular concentrate for warfarin) - in case of overdose.
coagulation (DIC) 10. Ensure a switch to another anticoagulant if apixaban,
edoxaban, dabigatran, or rivaroxaban is stopped
PHARMACOKINETICS suddenly for any reason other than pathological
bleeding - because of the risk of thromboembolic
events.
11. Monitor the patient carefully when any drug or herb is
added to or withdrawn from the drug regimen of a
patient taking warfarin - because of the risk of
T1/2 drug–drug interactions that would change the
- 30 to 180 minutes effectiveness of the anticoagulant

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

12. Make sure the patient receives regular follow-up and - cardiac arrhythmias (with coronary reperfusion)
monitoring, including measurement of clotting times, - - hypotension
to ensure maximum therapeutic effects. - hypersensitivity reactions
- Provide thorough patient teaching
- name of the drug, dosage prescribed
UROKINASE
- measures to avoid adverse effects
- warning signs of problems - converts endogenous plasminogen to plasmin →
- the need for periodic monitoring and breaks down fibrin clots, fibrinogen, and other plasma
evaluation proteins
- the need to wear or carry a MedicAlert - lyses thrombi and emboli
notification - used for lysis of PE or PE with unstable
to enhance patient knowledge about drug therapy and to hemodynamics in adults
promote compliance with the drug regimen.
ADVERSE EFFECTS
THROMBOLYTIC AGENTS - headache
- angioneurotic edema
- hypotension
DRUGS IN FOCUS - skin rash
1. Alteplase - bleeding
1. Reteplase - breathing difficulties
2. Tenecteplase - bronchospasm
3. Urokinase - pain
- fever
➢ break down the thrombus that has been formed by - anaphylactic shock
stimulating the plasmin system (clot resolution)
➢ activates conversion of plasminogen to plasmin → NURSING CONSIDERATION
breaks down fibrin threads and dissolves any formed IMPLEMENTATION
clot 1. Arrange to administer tissue plasminogen activators
to reduce mortality associated with acute MI as soon
PHARMACOKINETICS as possible after the onset of symptoms - because the
- given via IV timing for the administration of these drugs is critical
- cleared from body after liver metabolism to resolve the clot before permanent damage occurs
- can cross the placenta to the myocardial cells.
2. Discontinue heparin if it is being given before
CONTRAINDICATIONS administration of a thrombolytic agent unless
- presence of allergy specifically ordered for coronary artery infusion - to
- pregnancy prevent excessive loss of blood.
- recent surgery, active internal bleeding, 3. Mark the chart of any patient receiving this drug à to
cerebrovascular accident (CVA) within the last 2 alert medical staff that there is a potential for
months, aneurysm, obstetrical delivery, organ biopsy, increased bleeding
recent serious GI bleeding, rupture of a non 4. Provide increased precautions against bleeding
compressible blood vessel, recent major trauma during invasive procedures; use pressure dressings
(including cardiopulmonary resuscitation), known and ice; avoid IM injections; and do not rub
blood clotting defects, cerebrovascular disease, subcutaneous injection sites - to decrease excessive
uncontrolled hypertension blood loss caused by anticoagulation.
- hepatic disease 5. Monitor coagulation studies regularly; consult with the
prescriber - to adjust the drug dose appropriately.
CAUTIONS 6. Institute treatment within 6 hours after the onset of
- lactation symptoms of acute MI - to achieve optimum
therapeutic effectiveness.
ADVERSE EFFECTS 7. Evaluate the patient regularly for any sign of blood
- bleeding loss (petechiae, bleeding gums, bruises, dark-colored

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

stools, dark colored urine) - to evaluate the - monitor for: bleeding from any site and for the
effectiveness of the drug dose and to determine the development of direct hepatic injury
need to consult with the prescriber if bleeding
becomes apparent.
ANTIDOTES
8. Arrange to type and crossmatch blood in case of
serious blood loss that requires whole-blood ➢ VITAMIN K
transfusion. - reverse the effects of warfarin → normalize
9. Monitor cardiac rhythm continuously if the drug is clotting time
being given for acute MI - because of the risk of - promotes the liver synthesis of several
alteration in cardiac function; have life support clotting factors
equipment on standby as needed - anticoagulant-induced prothrombin
deficiency - 2.5 to 10 mg intramuscularly (IM)
or subcutaneously or, rarely, 25 mg IM or
subcutaneously
LOW-MOLECULAR WEIGHT HEPARINS
➢ FRESH FROZEN PLASMA
➢ inhibit thrombus and clot formation by blocking factors - for patient bleeding excessively and for
Xa and IIa faster response
➢ do not greatly affect thrombin, clotting, or the PT →
fewer systemic adverse effects ➢ PROTHROMBIN COMPLEX CONCENTRATE
➢ block angiogenesis - a blood product, infused IV to supply the
➢ prevention of clots and emboli formation after certain clotting factors needed to restore hemostatic
surgeries or prolonged bed rest balance
➢ given just before (or just after) the surgery and is - dosing is based on the patient’s INR
continued for 7 to 14 days during the postoperative
recovery process ➢ PROTAMINE SULFATE
➢ caution: avoid combining these drugs with standard - antidote to heparin overdose
heparin - dose of 1-mg IV protamine neutralizes 90
units of heparin derived from lung tissue or
DRUGS: 110 USP of heparin derived from the
1. Dalteparin intestinal mucosa
2. Enoxaparin - must be administered slowly, not to exceed
50 mg IV in any 10-minute period
- can cause potentially fatal anaphylactic
reactions
ANTICOAGULANT ADJUNCTIVE THERAPY
DRUGS:
1. Lepirudin
HEMORRHEOLOGIC AGENT
2. Protamine Sulfate
3. Prothrombin Complex Concentrate ➢ PENTOXIFYLLINE
4. Vitamin K - drug that can induce hemorrhage
- decreases platelet aggregation and
decreases the fibrinogen concentration in the
LEPIRUDIN
blood
- directly inhibits thrombin, blocking the - decrease blood clot formation and increase
thromboembolic effects of this reaction blood flow through narrowed or damaged
- developed to treat a rare allergic reaction to heparin vessel
(heparin-induced thrombocythemia with associated - effective in treating intermittent claudication
thromboembolic disease) - Adverse Effects: headache, dizziness,
- 0.4-mg/kg initial IV bolus followed by a continuous nausea, and upset stomach
infusion of 0.15 mg/kg for 2 to 10 day

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

- taken orally three times a day for at least 8 ● T1/2: 12 hours, cleared from the body by normal
weeks protein metabolism

ADVERSE EFFECTS
BLEEDING DISORDERS - allergic reaction
1. HEMOPHILIA - stinging at injection site
- A genetic lack of clotting factors that leaves - headache
the patient vulnerable to excessive bleeding - rash
with any injury - chills
2. LIVER DISEASE - nausea
- The clotting factors and proteins needed for - hepatitis
clotting are not produced - AIDS (risks associated with the use of blood products)
3. BONE MARROW DISORDERS
- Platelets are not formed in sufficient quantity NURSING CONSIDERATION
to be effective IMPLEMENTATION
1. Ensure that appropriate clotting factor is being used
for the patient - to ensure therapeutic effectiveness
and prevent inappropriate increase in other clotting
DRUGS USED TO CONTROL BLEEDING
factors.
2. Administer by the IV route only - to ensure therapeutic
effectiveness.
ANTIHEMOPHILIC AGENTS
3. Monitor clinical response and clotting factor levels
➢ replace clotting factors that are either missing or low regularly - to arrange to adjust dose as needed.
in a particular hemophilia 4. Mark the chart of any patient receiving this drug - to
alert medical staff that there is a potential for
DRUGS increased bleeding.
1. Antihemophilic Factor 5. Monitor the patient for any sign of thrombosis -
2. Antihemophilic Factor Fc Fusion Protein arrange to use comfort and support measures as
3. Antihemophilic Factor Porcine Sequence needed (e.g., support hose, positioning, ambulation,
4. Anti Inhibitor Coagulant Complex exercise).
5. Coagulation Factor Viiafactor IX 6. Decrease the rate of infusion if headache, chills,
6. Factor IX Complex fever, or tingling occurs - to prevent severe drug
7. Factor XIII Concentrate reaction; in some individuals, the drug will need to be
discontinued.
PHARMACOKINETICS 7. Arrange to type and crossmatch blood in case of
- given IV serious blood loss that requires whole-blood
- T1/2: 24-36 hours transfusion.

CONTRAINDICATIONS
- presence of known allergy to mouse proteins
HEMOSTATIC AGENTS
- FACTOR IX: presence of liver disease with signs of
intravascular coagulation or fibrinolysis
- Coagulation Factor VIIa: known allergies to mouse,
Topical Systemic
amster, or bovine products
- pregnancy & lactation
Absorbable Gelatin Human Aminocaproic Acid
Fibrin Sealant Microfibrillar
ANTIHEMOPHILIC FACTOR
Collagen Thrombin
● normal plasma protein that is needed for the
Thrombin, Recombinant
transformation of prothrombin to thrombin
● treatment of classic hemophilia → provide temporary
replacement of clotting factors to correct or prevent
bleeding episodes or to allow necessary surgery

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

- used to care of wounds or decubitus ulcers

AMINOCAPROIC ACID
- inhibits plasminogen-activating substances and has PHARMACOKINETICS
some antiplasmin activity - Absorbable Gelatin and Microfibrillar Collagen:
- used to prevent body-wide or systemic clot sponge form, applied directly to the injured area until
breakdown, thus preventing blood loss or the bleeding stops
hyperfibrinolysis - Human Fibrin Sealant: spray form and applied in a
thin layer onto the graft bed
DRUGS IN FOCUS: - Thrombin: from bovine sources, applied topically and
TOPICAL mixed in with the blood
1. Absorbable Gelatin - Thrombin Recombinant: applied directly to the
2. Human Fibrin Sealant bleeding site surface in conjunction with absorbable
3. Microfibrillar Collagen Thrombin gelatin sponge
4. Thrombin, Recombinant
SYSTEMATIC CAUTIONS
1. Aminocaproic Acid - allergy to bovine products
- children
PHARMACOKINETICS
- taken via oral and IV
- T1/2: 2 hours ADVERSE EFFECTS
- excreted largely unchanged in urine - pose a risk of infection
- rapidly absorbed and widely distributed throughout
the body NURSING CONSIDERATION
IMPLEMENTATION
CONTRAINDICATIONS 1. Monitor the patient for any sign of thrombosis - to
- Allergy arrange to use comfort and support measures as
- acute DIC needed (e.g., support hose, positioning, ambulation,
exercise).
CAUTIONS 2. Orient the patient and offer support and safety
- allergy measures if hallucinations or psychoses occur - to
- cardiac disease prevent patient injury.
- renal & hepatic dysfunction 3. Offer comfort measures - to help the patient deal with
- pregnancy the effects of the drug. These include small, frequent
- lactation meals, mouth care, environmental controls, and
safety measures
ADVERSE EFFECTS 4. Monitor clinical response and clotting factor levels
regularly - to arrange to adjust dose as needed.
● Dizziness ● Tinnitus
● Headache ● Weakness
● Hypotension ● Nausea DOSAGE AND CALCULATIONS
● Cramps ● Diarrhea
● Fertility Problems ● Malaise
● Elevated Serum MEASURING SYSTEMS
Creatinine
Phophokinase
1. THE METRIC SYSTEM
DRUG-DRUG INTERACTIONS
- development of hypercoagulation states if it is - the most widely used system of measure
combined with oral contraceptives or estrogen - It is based on the DECIMAL SYSTEM, so all units are
- risk for bleeding increases if it is given with heparin determined as multiples of 10. The system is used
worldwide, making sharing knowledge and research
TOPICAL HEMOSTATIC AGENTS information easier.

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

- The U.S. Pharmacopeia Convention 1995 established

standards requiring that all prescriptions be dispensed
2. THE APOTHECARY SYSTEM
only in METRIC FORM.
- Developed in the 18th Century Century, is the - has been used in England since the 17th century.
internationally accepted system of measure. - It is a very old measurement system developed for
use by the apothecaries or pharmacists.
THE BASIC UNITS OF MEASURE ARE:
1. GRAM (G,g, gm.) - for weight THE BASIC UNITS OF MEASURE ARE:
2. LITER (L) - for volume 1. MINIM - for liquid measure
3. METER (m, M) – for length 2. GRAIN - for solid measure
This system uses ROMAN numerals placed after the
PREFIXES INDICATE THE SIZE OF UNITS IN MULTIPLE unit of measure to denote the amount,
OF 10. Ex. 15gr (gr xv)
- KILO is the prefix used for larger units, while centi,
milli, micro, and nano are for smaller units. RULES FOR APOTHECARY CONVERSION
A. When converting LARGER units to SMALLER units
METRIC UNITS: used in most drug notations are; multiply the measurement that is requested by the
1. 1 gm = 1000 mg basic equivalent value.
2. 1L = 1000 ml
3 fluid oz.=______fluid dram convert 3qt =_____pint
3. 1mg = 1000 mcg
given : 1 fluid oz= 8 fluid dram. Given: 1 qt=2 pints
RULE FOR METRIC CONVERSION
A. When converting LARGER units to SMALLER units in
Hence: 3 fl oz x 8 fl dram=24 fl dram
a metric system move the decimal point 3 places to
3qt.x 2 pints. = 6 pints
the RIGHT.
1 kiloliter = 1.0>0>0. Liter
Hence 1 kl=1000 liters
B. When converting SMALLER units to LARGER units
1 kilogram= 1 .>0> 0>0. grams 1kg=1000 gm.
divide the requested number by the equivalent value.
8 fl oz=. _____pint
B. When converting SMALLER units to LARGER units
given: 1 pint=16 fl oz
move the decimal point 3 places to the LEFT.
Hence: 8 fl oz. divided by 16 = 0.5 pint or ½ pint
change 1000 mg to grams.
1000 mg = 1. <0<0<0 gm
APOTHECARY EQUIVALENTS
hence 1000 mg = 1 gm
DRY WEIGHT
METRIC EQUIVALENTS
1 OUNCE(OZ) 480 GRAINS /
1g 1000mg gr. 15 - 16 8 DRAMS

0.5 gm 500 mg gr 7.5

1 DRAM 60 GRAINS
0.3 gm 300 mg gr 5

0.1gm 100 mg gr .5 1 SCRUPLE 20 GRAINS

0.6 gm 60 mg gr 1
NOTE:
1 kg 2.2 pounds (lb) gr (from Latin granum) drop abbreviated as gtt (guttae)

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FINALS REVIEWER | MADE BY: Arabella Francisco & Joachim Fabi

FLUID VOLUME
RULE OF CONVERSION FOR HOUSEHOLD SYSTEM
A. When converting LARGER units to SMALLER units
1 PINT 16 FLUID OZ
multiply the number by the basic equivalent value.
e.g. 2 glasses =____oz. Given: 1 glass=8 oz.
1 QUART 2 PINTS 2 glasses x 8 oz=16 oz

1 FLUID OZ 8 FLUID DRAMS B. When converting SMALLER units to LARGER units

divide the number by the equivalent value.
e .g. 6 tsp =____ tbsp. Given 1 tbsp=3 tsp.
1 FL DRAM 60 MINIM 6 tsp divided by 3 (6/3)=2 tbsp.

1 MINIM 1 DROP (gtt)

1 CC 15 - 16 MINIMS
4. THE AVOIRDUPOIS SYSTEM
NOTE:
Minims used in eye/ear medications. (i means 1) - is another older system that was very popular when
pharmacists routinely had to compound medications.
- This system uses ounces and grains but they
measure differently than those of the apothecary and
household systems. It is seldom
3. THE HOUSEHOLD SYSTEM - Used by prescribers but may be used for bulk
medicines coming from the manufacturer.
- the measuring system that is found in recipe books. It
is commonly used in home and community settings.
- The measurement is approximate and not as accurate
as the metric system.
OTHER SYSTEMS
THE BASIC UNITS OF MEASURE ARE:
SOME DRUGS ARE MEASURED IN UNITS OTHER
1. teaspoon- the basic unit of fluid measure
THAN THOSE ALREADY DISCUSSED.
2. pound- the basic unit of solid measure
UNIT: usually reflects the biological activity of the
HOUSEHOLD EQUIVALENTS
drug in 1 ml of solution. The unit is unique for the drug it
1 CUP 8OZ measures, a unit of heparin is not comparable with a unit of
insulin.
1 GLASS 8 OZ 1. Milliequivalents (mEq): are used to measure
electrolytes (e.g., K, Na, Ca, flouride.) The
1 COFFEE CUP 6 OZ milliequivalents refer to the ionic activity of the drug .
2. International Units: are sometimes used to measure
1 OZ 2 TBSP. / 30 ML certain Vitamins or enzymes and are also unique to
each drug.
1 POUND (lb) 16 OZ
COMMONLY ACCEPTED CONVERSIONS BETWEEN
1 TSP 5 ML / 60GTTS SYSTEMS OF MEASUREMENT
I. SOLID MEASURE
1 TBSP 3 TSP
METRIC APOTHECARY HOUSEHOLD
1 GTT 1 MINIM SYSTEM

1 CC 1 ML 1 KG 2.2 lb

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1 GM / 1000 MG 15 gr (gr xv)

60 MG 1 gr (gr i)

30 MG ½ gr (gr ss)

454 G 1.0 lb

II. LIQUID MEASURE

METRIC APOTHECARY HOUSEHOLD 3 STEPS METHOD
SYSTEM

1 L / 1000 ML About 1 qt.

240 ML 8 fl. oz 1 CUP

30 ML 1 fl. oz 2 TBSP

15 - 16 ML 4 fl dr. 1 TBSP / 3TSP

8 ML 2 fl dr 2 TSP
INTERPRETING DRUG LABELS
- Pharmaceutical companies usually label their drugs
4- 5 ML 1 fl dr. 1 TSP / 60 GTT
with the brand name, also called the trade name and
the generic name.
1 ML 15 - 16 minim
- labels for generic drugs may have only the generic
name of the drug listed.
- the formulation or the drug amount per tablet or
capsule or unit of liquid is printed on the drug label.
other info. on drug labels, including lot #, expiration
CALCULATION METHODS
date, proper storage, or whether it is a controlled
3 General Methods of Drug Calculations substance.
1. Basic Formula [BF]
2. Ratio and Proportion [RP / FE - Fractional Equation] Precautions When Reading Drug Labels
3. Dimensional Analysis [DA] 1. BE AWARE 0F DRUG NAMES THAT SOUND OR
NOTE: above methods are used to calculate most enteral and LOOK ALIKE FOR
parenteral drug dosages. All but the DA requires using the EX: PERCODAN AND PERCOCET. (Percocet contains
same units of measure. oxycodone and acetaminophen while Percodan contains
oxycodone and aspirin)
Drugs that require individualized dosing, and calculation using 2. TO DECREASE MEDICATION ERRORS THE
the BSA and BW are used. These 2 methods are mostly used NURSE ADMINISTERING THE DRUG
for the calculation of the following: - should perform a minimum of 3 label checks
1. pediatric dosages with the Patient’s Medicine Administration
2. treatment of cancer (antineoplastic drugs) Record (Mar).
3. for individuals whose body weight is very low, obese
patients, or older adults. DRUG RECONSTITUTION
● drugs that come in powder or liquid form may need
FORMULA FOR COMPUTATION OF IV FLUIDS reconstitution. the liquid used to reconstitute a drug is
called a DILUENT.
● diluents can be nonsterile for enteral adm., sterile
water for injection 0.9% saline solution, or special fluid
supplied by the manufacturer.

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● the nurse must follow the manufacturers direction for 2. Quantities less than 1 are rounded to the nearest
reconstitution hundredth.
Example: 0.825 = 0.83 ; 0.823 = 0.82
METHODS OF CALCULATING DRUG DOSES
ORAL MEDICATIONS
A. BASIC FORMULA 1. A capsule cannot be divided.
2. Tablets that are scored (a line marked on the tablet)
may be divided
3. If the oral medication is a liquid, the nurse checks to
see if it is possible to administer an accurate dosage

PARENTERAL MEDICATIONS
1. Rounding depends on the amount (i.e., less than or
more than 1) and the syringe used.

IV INFUSION
1. By gravity: Round to the nearest whole number.
2. By IV pump: If the IV pump uses only whole number,
round to the nearest whole number.Some IV pumps
used in critical care units can be set to a tenth of a
B. RATIO AND PROPORTION
rate (e.g., 11.8 mL/h). Round to the nearest tenth
decimal point.

Rounding Down
To round down...
- Hundredths, drop all the numbers after the hundredth
place
- For tenths, drop all the numbers after the tenth place,
- Whole number, all the numbers after the decimal.
For example, 6.6477 rounded down all the nearest Hundredth
= 6.64; Tenth = 6.6; Whole number = 6

C. DIMENSIONAL ANALYSIS METHOD

- used when one unit of measurement is converted to
an equivalent quantity in a different unit of
FIVE METHODS USED TO CALCULATE DRUG DOSAGE measurement.

6 STEPS
I. Basic Formula Method
1. Identify the dose on hand
II. Ratio and Proportion Method
2. Identify the desired dose.
III. Body Weight Method
3. Write down the conversion factor, if needed.
IV. Body Surface Area Method
4. Set up the equation
V. Dimensional Analysis Method
5. Cancel units that appear in the numerator and
denominator
Guidelines in Rounding Numbers 6. Multiply the numerator. Multiply the denominator.
Divide the products.
GENERALLY..
EXAMPLES:
1. Quantities greater than 1 are rounded to the nearest
WITHOUT A CONVERSION FACTOR:
tenth.
Order: Valsartan 120 mg
Example: 1.67 = 1.7 ; 1.63 = 1.6
On Hand: Valsartan 40 mg tablets

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3 STEPS
How many capsules of Valsartan will you administer? 1. Convert pounds to kilograms
2. Determine the drug dose per body weight by
multiplying drug dose x body weight x frequency.
3. Choose a method of drug calculation to determine the
amount of medication to administer.

EXAMPLE:
Order: Keflex, 20mg/kg/day in three divided doses. The client
weighs 20 pounds
On hand: Keflex oral suspension 125 mg per 5 mL

How many mL of Keflex will you administer per dose?

USING A CONVERSION FACTOR

Order: Dofetilide 0.5 mg
On Hand: Dofetilide 125 mcg capsules

How many capsules of Defetilide will you administer?

E. BODY SURFACE AREA METHOD

The formula is the ratio of the child’s body surface area to the
surface area of an average adult (1.7 square meters, or 1.7 m2
), multiplied by the normal adult dose of the drug:

EXAMPLE:
For example, a child who weighs 10 kg and is 50 cm tall has a
body surface area of 0.4 m2.
What is the child’s dose of tetracycline corresponding
D. BODY WEIGHT METHOD to an adult dose of 250 mg?
● Given Values: SA of Adult = 1.7 m2

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● SA of Child = 0.4 m2 Calculate the correct setting (drops per minute)

● Normal Adult Dose = 250 mg

INTRAVENOUS SOLUTIONS
Intravenous (IV) solutions are used to deliver a
prescribed amount of fluid, electrolytes, vitamins, nutrients, or
drugs directly into the bloodstream.

I. Electronic Infusion Pump

EX. You are preparing to administer 1 gram of cefotaxime as IV
bolus over 45 minutes. The cefotaxime is available in 100mL of
0.9% sodium chloride.

How many mL/h should you set the IV infusion pump to

deliver? Round to the nearest whole number.

METHODS:
1. Ratio and Proportion and Desired Over Have
Methods If a patient has an order for an IV drug, the same principle can
be used to CALCULATE THE SPEED OF THE DELIVERY.
X mL / h = 𝑣𝑜𝑙𝑢𝑚𝑒 (𝑚𝐿) / 𝑡𝑖𝑚𝑒 (ℎ)
For example, an order is written for a patient to receive 50 mL
Put in the numbers that are known from the example and solve of an antibiotic over 30 minutes. The IV set used dispenses 60
for X. drops/mL, which allows greater control. Calculate how fast the
X mL / h = 100 mL /0.75 h delivery should be.
X mL / h = 133.333 mL / h
This rounds to 133 mL / h

2. Dimensional Analysis Method

II. Manual IV Infusion

An order has been written for a patient to receive 400 mL of
5% dextrose in water (DSW) over a period of 4 hours in a
standard microdrip system (i.e., 60 drops/mL).

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↓
circulating LPL is reabsorbed to be processed
LIPID LOWERING AGENTS

DRUGS IN FOCUS
1. Cholestyramine
- adjunctive therapy of primary
hypercholesterolemia that has not
responded to dietary modifications
- tx of pruritus associated with partial biliary
obstruction

2. Colestipol
- adjunctive therapy of primary
hypercholesterolemia

3. Colesevelam
- adjunctive tx with diet and excercise to
reduce LDL in adults
- Reduction of LDL in pediatric patients with
heterozygous familial hypercholesterolemia

PHARMACOKINETICS
- action limited in the GIT
- metabolized in the liver
- rapidly absorbed
- excretion through the feces

CONTRAINDICATIONS
1. allergy
AGENTS 2. biliary obstruction
1. Bile Acid Sequestrants
CAUTIONS
2. HMG-COA Reductase Inhibitors
1. intestinal problems
3. Cholesterol Absorption Inhibitor
2. pregnancy and lactation
4. PCSK9 Inhibitors

ADVERSE EFFECTS
BILE ACID SEQUESTRANTS CNS
- anxiety
- drowsiness
BILE: produce in the liver and stores in the gallbladder.
- muscle pains
GI SYSTEM
ACTION:
- fecal impaction
- aggravation of hemorrhoids
binds with bile acids in the intestine to form an insoluble
- vitamin a & d efficiency
complex
BLEEDING
↓
- decrease vit. K absorption
bile acid is used up and cholesterol is excreted
(increases bleeding time)
↓
- decrease production of clotting factors
stored cholesterol in the liver is processed to make more bile
acids
DRUG INTERACTIONS
↓
a. malabsorption of fat soluble vitamins
hepatic intracellular cholesterol level fats

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b. decrease or delay absorption of thiazide diuretics, CNS

warfarin, thyroid hormones, hormonal contraceptives, - headache
and corticosteroids. - dizziness
c. should be taken 1hr before or 4-6hrs after the bile - blurred vision
acid sequestrant - insomnia
d. cholestyramine and colestipol: mixed powder form - fatigue
with fruit juice, liquids, cereals, or pulpy fruits OTHER
- increased of liver enzymes
- rhabdomyolysis
HMG-COA REDUCTASE INHIBITORS
Full: Hydroxy-Methyl-Glutaryl Coenzyme A Reductase DRUG INTERACTIONS
Inhibitors a. medications that suppress CYP3A4 and ezetimibe
- can increase levels of statins in the serum
ACTION - increase risk of mypopathy and liver
complete synthesis with cholesterol impairment
↓ b. avoid drinking grapefruit juice while taking these
block hmg-coa reductase drugs - can increase serum levels
↓
block synthesis of cholesterol in the liver
CHOLESTEROL ABSORPTION INHIBITOR
↓
lowers cholesterol and lpl levels
ACTION
work in the small intestine and decrease absorption of dietary
cholesterol in the small intestine
DRUGS IN FOCUS ↓
1. Atorvastatin Less dietary cholesterol is delivered in the liver
2. Fluvastatin ↓
3. Rosuvastatin Increase clearance of cholesterol in the liver
↓
PHARMACOKINETICS Liver increases clearance of cholesterol from the circulation
- absorbed in the GIT
- distributed in the liver
- metabolized in the liver DRUGS IN FOCUS
- excretion through feces and urine 1. Ezetimibe

CONTRAINDICATIONS PHARMACOKINETICS
- allergy - absorbed well
- any beta - distribution and metabolized through the small
- liver impairment intestine and liver
CAUTIONS - excretion through the feces and urine
- pregnancy
- impaired endocrine function CONTRAINDICATION
- allergy
ADVERSE EFFECTS - liver impairment
GI SYSTEM
- flatulence CAUTIONS
- abd. pain - pregnancy and lactation
- cramps
- nausea ADVERSE EFFECTS
- vomiting GI
- constipation - diarrhea
LIVER

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- rare case leads to hepatitis

RESPIRATORY II. VITAMIN B3
- respiratory tract infection - known as Niacin
- inhibits the release of fatty acids from
DRUG INTERACTIONS adipose tissues
a. administration with bile sequestrants - interferes with - increases the rate of triglyceride and removal
absorption; ezetimibe should be taken 2hrs before or from plasma
after 4hrs after a bile sequestrant - reduces LDL and triglyceride levels and
b. taken with cyclosporine and fibrates = elevated serum increases HDL levels
levels
c. fibrates = increase cholelithiasis (gallstones) III. OMEGA 3 FATTY ACIDS
- inhibits liver enzyme systems to decrease
the synthesis of triglycerides, a risk factor in
PCSK9 INHIBITORS
metabolic syndrome, lowering serum
Full: Proprotein Convertase Subtilisin/Kexin Type 9 triglyceride levels

ACTION IV. OTHER THERAPIES

bind to pcsk9 enzymes and inhibits attachment to the lpl - Suxtapin: not used due to hepatoxicity
receptors on the liver cell
↓
GIT DRUGS
more LPLis processed in the liver
↓
decrease LDL levels in the plasma
DRUGS AFFECTING GI SECRETIONS

DRUGS IN FOCUS
Drugs Used To Treat Gastroesophageal Reflux Disease
1. Alirocumab
and Ulcer Disease
2. Evolucumab

PHARMACOKINETICS I. HISTAMINE - 2 ANTAGONISTS

- absorbed well after subcutaneous injection - block the release of hydrochloric acid in
- metabolized in the liver and small intestine response to gastrin
- distributed in the circulatory system DRUGS:
- excretion in the feces and urine 1. Cimetidine
2. Famotidine
CONTRAINDICATIONS 3. Nizatidine
- allergy (latex allergy) 4. Ranitidine

ADVERSE EFFECTS THERAPEUTIC ACTIONS AND INDICATIONS

- urinary tract infection H2 antagonists selectively block H2 receptors located
- nasopharyngitis on the parietal cells. Blocking these receptors prevents 70% of
- upper respiratory tract infection hydrochloric acid release from parietal cells.
- influenza - short term tx of active duodenal ulcer to benign
gastric ulcer
- tx of pathological hypersecretory conditions
OTHER LIPID LOWERING AGENTS
- prophylaxis of ulcers induced by stress or nsaid
I. FIBRATES - tx of erosive gastroesophageal reflux
- stimulates the breakdown of lipoproteins - tx of ulcers caused by h. pylori
from the tissues and their removal from the - relief of symptoms of heartburn and indigestion
plasma
- lead to decrease in lipoprotein and
triglyceride synthesis and secretion

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PHARMACOKINETICS DRUG-DRUG INTERACTIONS

➢ Cimetidine ★ Cimetidine can slow the metabolism of other drugs
- only in oral form leading to increased serum levels
- first drug in this class to be developed ★ Nizatidine if taken with aspirin - risk of increased
- associated with antiandrogenic effects salicylate
- peak level 1-1.5 hrs
- metabolized mainly in the liver; can slow the
metabolism of many drugs II. ANTACIDS
- excreted in the urine - group of inorganic chemicals that neutralize stomach
- cross placenta and enter human milk acid
- available OTC
➢ Famotidine DRUGS:
- available in oral and parental form 1. Aluminum Salts
- peak effect 1-3hrs; duration of 6-15 hrs. 2. Calcium Salts
- metabolized in the liver 3. Magnesium Salts
- excreted in the urine 4. Sodium Bicarbonate
- cross placenta and enter human milk
- approved for use in children 1-16yrs. THERAPEUTIC ACTIONS AND INDICATIONS
Neutralize stomach acid by direct chemical reaction.
➢ Nizatidine - symptomatic relief of an upset stomach associated
- only in oral form with hyperacidity
- newest drug in this class - hyperacidity associated with peptic ulcer
- eliminated in the kidneys with no first-pass - gastritis
metabolism in the liver - peptic esophagitis
- for patients with liver dysfunction - gastric hyperacidity
- cross placenta and enter human milk - hiatal hernia

➢ Ranitidine PHARMACOKINETICS
- recalled by the FDA in 2020 and not ➢ Sodium bicarbonate
available in the US. - oldest drug in this class
- available in many preparations (e.g. baking
CONTRAINDICATIONS AND CAUTIONS soda powder, tablets, solutions, injectable)
- allergy - widely distributed when absorbed orally
- pregnancy and lactation - peak level 1-3hrs
- hepatic and renal dysfunction - excretion urine
- can cause serious electrolyte imbalance in
ADVERSE EFFECTS people with renal impairment
GI EFFECTS
1. diarrhea CONTRAINDICATIONS AND CAUTIONS
2. constipation - allergy
CNS EFFECTS CAUTION:
1. Dizziness 1. any condition that can be exacerbated by electrolyte
2. Headache or acid-base imbalance
3. Somnolence 2. GI obstruction
4. Confusion 3. Renal dysfunction
5. Hallucinations 4. Pregnancy and lactation
OTHERS
1. cardiac arrhythmias ADVERSE EFFECTS
2. hypotension - acid-base imbalance
- acid rebound (increase acid production)
- alkalosis with resultant metabolic change (nausea,
vomiting, headache, neuromuscular changes etc.)

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- calcium salts = hypercalcemia and milk-alkali ADVERSE EFFECTS

syndrome CNS EFFECTS
- constipation and diarrhea 1. Dizziness
- aluminum salts = hypophosphatemia 2. Headache
- sodium bicarbonate = fluid retention and heart failure 3. Asthenia (loss of strength)
4. Vertigo
DRUG-DRUG INTERACTIONS 5. Insomnia
- affect the absorption of drugs in the GI tract 6. Apathy
7. Dream Abnormalities
GI EFFECTS
III. PROTON PUMP INHIBITORS 1. Diarrhea
- suppress the secretion of hydrochloric acid into the 2. Abd pain
lumen of the stomach 3. Nausea and vomiting
4. Dry mouth
DRUGS: 5. Tongue atrophy
1. Dexlansoprazole UPPER RESPIRATORY
2. Esomeprazole 1. Cough
3. Lansoprazole 2. Stuffy nose
4. Omeprazole 3. Hoarseness
5. Pantoprazole 4. Epistaxis
6. Rabeprazole LESS COMMON
1. Rash
THERAPEUTIC ACTIONS AND INDICATIONS 2. Alopecia
suppress gastric acid secretion by specifically 3. Pruritus
inhibiting the hydrogen-potassium adenosine triphosphate; the 4. Dry skin
action blocks the final step of acid production, lowering the acid 5. Back pain
levels in the stomach 6. Fever
- short term tx of active duodenal ulcers
- gerd DRUG-DRUG INTERACTIONS
- erosive esophagitis 1. taken with benzodiazepines, phenytoin and warfarin =
- benign active gastric ulcer risk of increased serum levels and increased toxicity
- long term tx of pathological hypersecretory conditions 2. decreased levels of ketoconazole and theophylline
- maintenance therapy for healing of erosive
esophagitis IV. GASTROINTESTINAL PROTECTANT
coat any injured area in the stomach to
PHARMACOKINETICS prevent further injury from acid
- acid labile
- rapidly absorbed in the GI tract DRUG:
- peak level 3-5 hrs. 1. Sucralfate
- undergo extensive metabolism in the liver
- excreted in the urine THERAPEUTIC ACTIONS AND INDICATIONS
- no adequate studies whether these drugs crosses the - forms an ulcer-adherent complex at duodenal ulcer
placenta and human milk sites
- prevents further breakdown of the area
● Omeprazole - faster acting and more quickly excreted - promotes ulcer healing
● Esomeprazole - longer acting drug - prevents further breakdown on proteins in the
stomach
CONTRAINDICATIONS AND CAUTIONS
- allergy PHARMACOKINETICS
- CI to be used concurrently with medications - minimally absorbed after oral administration
containing RILPIVIRINE - most is excreted via the feces; small amount excreted
- pregnancy and lactation in the urine

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- no harm in pregnancy ADVERSE EFFECTS

- nausea
CONTRAINDICATIONS AND CAUTIONS - diarrhea
- allergy - abd pain
- renal failure - flatulence
- undergoing dialysis - vomiting
- pregnant and lactating women - dyspepsia
- constipation
ADVERSE EFFECTS - miscarriages
GI EFFECTS - excessive bleeding spotting
1. Constipation - other menstrual disorders
2. Diarrhea
3. Nausea
4. Indigestion
ANTIEMETIC DRUGS
5. Gastric Discomfort
6. Dry Mouth
Key Terms:
` OTHER
1. Dizziness ANTIEMETIC- agents that blocks innervation of the vomiting
2. Vertigo center to decrease the symptoms of nausea and vomiting
3. Skin Rash EMETIC- agents used to induce vomiting to rid the stomach of
4. Back Pain toxins or drugs
INTRACTABLE HICCOUGH- repetitive stimulation of the
DRUG-DRUG INTERACTIONS diaphragm that leads to hiccough, a diaphragmatic spasms
- Aluminum Salts = risk of high aluminum levels and that persist over time
toxicity
- Phenytoin, digoxin, warfarin, fluoroquinolone, I. PHENOTHIAZINES
antibiotics, penicillamine = decreased serum levels - are centrally acting antiemetics that change
and drug effectiveness the responsiveness or stimulation of the cTz
- Administered separately for at least 2hrs. in the medulla

V. PROSTAGLANDINS DRUGS:
protect the stomach lining 1. Chlorpromazine
2. Perphenazine
THERAPEUTIC ACTIONS AND INDICATIONS 3. Prochlorperazine
inhibits gastric acid secretion and increases bicarbonate and
mucus production in the stomach THERAPEUTIC ACTIONS AND INDICATIONS

DRUGS: Misoprostol The phenothiazines are recommended for the treatment of:
- nausea and vomit-ing, including that specifically
PHARMACOKINETICS associated with anesthesia
- Oral - severe vomiting
- Rapidly absorbed from GI tract - intractable hiccoughs, which occur with repetitive
- Metabolized in the liver stimulation of the diaphragm and lead to persistent
- Excreted in the urine diaphragm spasm.
- Cross placenta and human milk
PHARMACOKINETICS:
CI AND CAUTIONS Available:
- Allergy - Tablets
- Pregnancy and lactation - Syrup
- Hepatic and renal impairment - Rectal suppositories
- Solutions (IV and IM)

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DRUG:
Onset: 5-20 minutes 1. Metoclopramide (Reglan)
Duration: 3-12 hours - Blocking dopamine receptors and making GI cells
Metabolized: liver sensitive to acetylcholine
Excreted: Urine INDICATIONS:
Crosses placenta and enters human milk Relief of symptoms of gastroesophageal reflux disease,
prevention of nausea and vomiting after emetogenic
CONTRAINDICATIONS AND CAUTIONS: chemotherapy or postoperatively, relief of symptoms of diabetic
- coma and severe CNS depression gastroparesis, promotion of GI movement during small bowel
- brain damage and injury intubation or promotion of rapid movement of barium.
- severe hypotension and hypertension
- liver dysfunction ADVERSE EFFECTS:
Cautions to: - drowsiness
- renal dysfunction or impairment - fatigue
- active peptic ulcers - restlessness
- pregnancy and lactation - extrapyramidal symptoms
- Promethazine: contraindicated to pediatric patients - Parkinsons-like reactions
younger than 2 years - seizures
- nausea
ADVERSE EFFECTS: - diarrhea
CNS
- drowsiness III. 5-HT3 RECEPTOR BLOCKERS
- dizziness - Blocks those receptors associated with
- weakness nausea and vomiting in the CTZ and locally
- Tremor
- headache DRUGS:
Others: 1. granisetron (Sancuso, Sustol)
- hypotension 2. ondansetron (Zofran)
- cardiac arrhythmia 3. palonosetron (generic)
AUTONOMIC
- dry mouth THERAPEUTIC ACTIONS AND INDICATIONS:
- nasal congestion - The 5-HT3 receptor blockers have proven especially
- anorexia helpful in treating the nausea and vomiting
- pallor associated with anti-neoplastic chemotherapy and
- sweating radiation therapy and postoperative nausea and
- urinary retention (tinged pink to red-brown urine) vomiting. They are specific for the treatment of
ENDOCRINE nausea and vomiting associated with emeto-genic
- menstrual disorder chemotherapy. They are approved for use in children
- galactorrhea and adults.
- gynecomastia
PHARMACOKINETICS:
Others:
- Photosensitivity - Absorbed rapidly
- Peak level: within 1 hour
DRUG-TO-DRUG INTERACTIONS: - Metabolized: liver
- Excreted: urine
1. Antiemetics+CNS depressant & antihypertensives=
additive CNS depression and hypotension Ondansetron and Granisetron:
- available in oral and IV form
- granisetron is also available in transdermal
II. NON PHENOTHIAZINE formulation
Palonosetron:

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- available ONLY in IV forms

CONTRAINDICATIONS AND CAUTIONS:
ADVERSE EFFECTS: - There are no sufficient data to inform the risk if used
- headache during pregnancy and lactation. The medications
- dizziness should not be used if known allergy to any
- myalgia related to their CNS effects component of the drug to prevent hypersensitivity
- Pain at the injection site reactions.
- rash - Rolapitant cannot be combined with thioridazine or
- constipation pimozide.
- diarrhea - Aprepitant and Ensaprepitant should not be used
- hypotension with pimozide.
- urinary retention
ADVERSE EFFECTS:
DRUG-TO-DRUG INTERACTIONS: - diarrhea, constipation, and gastritis; nausea;
- Concurrent use with serotonergic medications can anorexia; headache; and fatigue. There can also be
increase risk of serotonin syndrome. Use of neutropenia, anemia, and leukopenia.
ondansetron with other QT-prolonging
medications can increase risk of torsade de
pointes.
RELY ON BOOK !!
IV. SUBSTANCE P/NEUROKININ 1 RECEPTOR
ANTAGONIST
- the newest class of drugs for treating nausea and
vomiting

DRUGS:
1. aprepitant
2. fosaprepitant dimeglumine
3. rolapitant

THERAPEUTIC ACTIONS AND INDICATIONS:

- act directly in the CNS to block receptors associated
with nausea and vomiting with little to no direct on
serotonin, dopamine, or corticosteroid receptor
- Aprepitant is approved for use in treating the nausea
and vomiting associated with highly emetogenic
antineoplastic chemotherapy, including cisplatin
therapy. It is given orally in combination with
dexamethasone.
- Fosaprepitant is a prodrug of aprepitant, so the
effects are due to the actions of aprepitant. It is
indicated for treatment of acute and delayed nausea
and vomiting associated with cancer chemotherapy.
- Rolapitant is used in combination with other
antiemetics for prevention of delayed nausea and
vomiting associated with emetogenic antineoplastic
chemotherapy.

PHARMACOKINETICS:
- metabolized in the liver
- excreted in the urine and feces
- cross the placenta and to enter human milk

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