PHARMACOLOGY

Doctor of Dental Medicine

3rd Year, 1st SEM Prelims UNDAG, SHIHKIA

D. IDIOSYNCRATIC REACTION
DRUG – DRUG INTERACTIONS
Drugs may interact by acting at the same receptor or • Type A ADRs
signal transduction pathway or more commonly, a drug • Type B ADRs
may affect the pharmacokinetics or another drug.
TOXICITY – results when the dose of the drug is
A. Induction of Metabolism – is a reaction to excessive for the particular patient.
certain drugs in which the number of liver
enzymes increases, resulting in a reduction in SIDE EFFECT – an adverse effect that occurs within the
the effect of the other drug. therapeutic dose range of the drug.

B. Inhibition of Metabolism – is a process by DRUG ALLERGY – an adverse effect due to an

which one drug either competes for metabolism immune reaction to a drug.
of another or directly inhibits drug-metabolizing
enzymes. IDIOSYNCRATIC REACTION – an adverse drug
reaction that is due to a genetic change usually involving
GENETICS AND PHARMACOLOGY a change in enzyme activity.
• Enzymes characteristics are important in
determining the response to a drug. IDIOSYNCRATIC REACTIONS TO DRUGS USED IN
• The rate of drug metabolism can vary greatly DENTISTRY
depending on cytochrome P450 isozyme profile of
the patient. GENETIC DRUGS IDIOSYNCRATIC
ABNORMALITY AFFECTED RESPONSE
NADH- Benzocaine, Methemoglobinemia
EXAMPLES OF DRUG-DRUG INTERACTIONS methemoglobin Prilocaine
IMPORTANT IN DENTISTRY reductase
deficiency
DENTAL INTERACTING Glucose-6- Aspirin, Hemolytic anemia
COMMENTS phosphate Primaquine,
DRUG DRUG
dehydrogenase Sulfonamides
Penicillin Macrolides, Bacteriostatic deficiency
tetracyclines, drugs reduce the
Abnormal heme Barbiturates, Porphyria
clindamycin effect of
synthesis Sulfonamides
bacteriocidal drugs
Low plasma Procaine and other Local anesthetic
Tetracyclines Oral Antacids Reduced
cholinesterase ester local toxicity
absorption of
activity anesthetics
tetracyclines
Altered muscle Volatile inhalation Malignant
Aspirin Anticoagulants Increased bleeding
calcium anesthetics, hyperthermia
tendency
homeostasis succinylcholine
Aspirin Probenecid Decreased effect of
probenecid
Aspirin Methotrexate Increased HYPERSENSITIVITY REACTIONS
methotrexate
toxicity ✓ TYPE I – reactions of anaphylactic reactions
Acetaminophen Alcohol Increased risk of
liver toxicity in (immediate hypersensitive reaction).
chronic alcoholics ✓ TYPE II – reactions or cytotoxic reactions.
Local Anesthetics Cholinesterase Antagonism of ✓ TYPE III – reactions or immune complex mediated
Inhibitors cholinesterase reactions. 1x
inhibitor – reduced
effectiveness of the
✓ TYPE IV – reactions or cell mediated reactions
cholinesterase (delayed hypersensitive reactions).
inhibitor in the
patient with
myasthenia gravis ESSENTIAL AND ORPHAN DRUGS
• Satisfy healthcare of majority of population
ADVERSE DRUG REACTIONS • Treat prevention, diagnosis and treatment of a rare
Undesired or unintended effect of the drug occurs at disease
dose normally used by human being.

A. TOXICITY
B. SIDE EFFECTS
C. DRUG ALLERGY
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 PHARMACOLOGY
Doctor of Dental Medicine
3rd Year, 1st SEM Prelims UNDAG, SHIHKIA

2 Major Types of Histamine

DRUG TESTING PHASES
1. H1 Receptors – when stimulated it
I Uses normal volunteers. Safety, results in smooth muscle
pharmacokinetics, etc., are assessed. contraction, increased vascular
permeability, and mucus
II Uses patients who could benefit from the drug. production.
Clinical efficacy, pharmacokinetics, and safety
are assessed. 2. H2 Receptors – when activated it
increases gastric acid production,
III Uses larger number of patients often involving and this effect is blocked by H2
several medical centers. Safety and clinical blockers such as cimetidine.
efficacy are assessed.
Classification of H1 receptor antagonists
IV Post-marketing surveillance. Safety, patterns
of use and new indications are assessed. 1. Potent and sedative: such as
diphenhydramine and promethazine.
AUTOCOIDS 2. Potent but less sedative: such as
cyclizine and chlorpheniramine.
• AUTOCOIDS (Greek “self-remedy”) 3. Less potent and less sedative: such as
• It is a collective term for various endogenous pheniramine.
peptides, prostaglandins, leukotrienes, and 4. Non-sedative: such as terfenadine,
cytokinesis. loratadine, and cetirizine.

1, Histamine – it is a potent tissue amine widely 2. 5-Hydroxytretptamine (serotonin) – widely

distributed in plant and animal tissues in the distributed in plants and animals.
venoms of bees. It has no valid therapeutic use - highest concentration in mammals is found in
currently, but it plays an important role in the pineal gland. Acts as a precursor for
anaphylaxis and other forms of allergic melatonin.
reactions. Major portion, stored in mass cells. - Causes constriction of renal, splanchnic,
meningeal, and pulmonary arteries and veins
- Its release may be included by various and venules, but dilatation of the blood vessels
agents including certain venoms, drugs, of skeletal muscles, coronaries, and skin
trauma (thermal, chemical, radiation), capillaries.
antigen-antibody reactions. - Altered functions may be responsible for
- In Cardiovascular System, histamine disturbances in sleep, mood, sexual behavior,
produces dilatation of capillaries and motor activity, pain perception, migraine,
venules. temperature regulation, endocrine control,
- In Smooth Muscles, histamine directly psychiatric disorders, and extra-pyramidal
stimulates the smooth muscles of various activity.
tissues including the bronchi and uterus.
- In Exocrine Glands, it is a powerful SEROTONIN AGONISTS
stimulant of HCI secretion by the gastric 1. Sumatriptan – a selective agonist of 5-HT1
mucosa. Hydrochloric acid in the gastric receptors. Highly effective in treating acute
juice breaks down the food and the attacks of migraine.
digestive enzymes and proteins. Gastric
juice also kills the bacteria. 2. Buspirone – is a useful effective anxiolytic
- In CNS, commonly known as “waking agent.
amine”. Acting by “increasing the sensitivity
of large cerebral areas to excitation inputs”. SEROTONIN ANTAGONISTS
Amines are commonly derivatives of 1. Methysergide – blocks the actions of 5-
ammonia. HT on a variety of smooth muscles.
- Miscellaneous actions: induction of Effective prophylactic agent for
itching and pain. migrainous headaches.
2. Cyproheptadine – a potent antagonist
of 5-HT and to a smaller extent of
histamine and acetylcholine.
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 PHARMACOLOGY
Doctor of Dental Medicine
3rd Year, 1st SEM Prelims UNDAG, SHIHKIA

3. Ondansetron – is a specific 5-HT3

receptor antagonist.
4. Prochlorperazine
5. Haloperidol

3. Prostaglandins – human seminal fluid is the richest

known source, but they are also present in
various tissues.
- are synthesized from polyunsaturated fatty
acids at their sites of action.
- PG E2 and PG F2 are the two main
prostaglandins.

ANTIHISTAMINIC DRUGS

• These drugs competitively block histamine

receptors.
- H1 receptor antagonists
- H2 receptor antagonists (used for treating
acid peptide disease)

H1 RECEPTOR ANTAGONISTS
▪ Anti-histaminic actions: they block histamine
effects at various sites.
▪ Are well-absorbed following oral and parenteral
administration. An are mainly metabolized by
the liver
Diseases – urticaria, seasonal hay fever, atopic
and contact dermatitis, mild blood transfusion
reaction.