final Flashcards by Marianne Nadeen Aini Tupay

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antagonism

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When a drug inhibits or counters or offsets the effect of another drug.

antagonism

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When 2 drugs combine in solution so that the effect of the active drug is lost

Chemical antagonism – Neutralization

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Type of chemical antagonism where the result is a reduction of the concentration of the active drug at its site of action

Pharmacokinetic antagonism

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Object drug (agonist) competes with the precipitant drug (antagonist) for the same receptor.

Pharmacologic: Competitive antagonism

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antagonist activity is reduced or cancelled when the agonist concentration is increased.

Reversible competitive antagonism

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the action of the antagonist is reversed by increasing the agonist concentration.

The antagonist dissociates very slowly from the receptor.

Irreversible antagonism

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The precipitant drug (antagonist) blocks the action of the object drug (agonist) at some point in the chain of events leading to the production of a response to the agonist.

Pharmacologic: Non-competitive antagonism

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When the action of the precipitant drug offsets the action of the object drug.

Physiological antagonism

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Nifedipine and verapamil prevent the influx of Ca++ ions through the cell membrane blocking the contraction of smooth muscle produced by other drugs

Pharmacologic: Non-competitive antagonism

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Phenobarbital induces metabolism of warfarin resulting in the reduction of plasma concentration of warfarin and reduced anticoagulant.

Pharmacokinetic antagonism

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Dimercaprol chelating with heavy metals and thus reduce their toxicity

Chemical antagonism – Neutralization

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Caffeine offsetting effect of depressants

Physiological antagonism

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Histamine stimulates GI acid secretion while omeprazole inhibits proton pump resulting in reduced acid secretion

Physiological antagonism

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Thiazide diuretics elevate blood glucose offsetting the effect of oral hypoglycemic drugs

Physiological antagonism

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Depressants counteracting effect of stimulants.

Physiological antagonism

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Caffeine Object Drugs

CNS Depressant
Aspirin
Theophylline
Ciprofloxacin
Cimetidine
Oral contraceptives
Prednisone

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Milk, Dairy products, Multivitaminsc Antacids, Food containing Ca, Mg, Al Object Drugs

Tetracycline
Bisacodyl

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Leafy green veggies – rich in vitamin K and Cranberry juice Object Drug

Warfarin

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Theobromine object drug

CNS Depressants

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Grapefruit juice object drugs

Many drugs

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Tyramine-rich food • Cheese, Red wine object drug

MAO Inhibitors

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Histamine – rich food object drugs

Isoniazid, MAOI

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Protein – rich food object drugs

Propanolol

Carbidopa/levodopa and theophylline

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High fat meal object drug

Griseofulvin

Fiber Object drugs

Metformin Digoxin Levothyroxine Penicillin

Fruit juice rich in vit. C object drug

Amphetamine

Alcohol object drug

Warfarin

Herbal drugs with anticoagulant object drug

Feverfew Garlic Ginkgo Biloba

Herbal drug with Phenelzine and Digoxin object drugs

Ginseng

Herbal drug with sedatives as object drug

Valerian (anti anxiety)

Herbal drug with heparin as object drug

Chondroitin

Herbal drug with hypolipidemics as object drug

Coenzyme Q10

Herbal drug with fluoxetine as object drug

Glucosamine

Melatonin object drugs

Vit. B12 MAOI, SSRI Beta blockers

Decrease secretion

melatonin - beta blockers

Increase plasma concentration

melatonin - maoi, ssri glucosamine - fluoxetine

Increase melatonin secretion

melatonin - vit b12

Lowers its plasma concentration

coenzyme q10 - hypolipidemics

Potentiation

valerian (anti anxiety) - sedatives

decrease plasma levels

st john’s wort (anti anxiety) - Antiretroviral, cyclosporine digoxin, theophylline and oral contraceptives

Decrease INR (international normalized ration) of warfarin

st john’s wort - warfarin

Cause serotonin syndrome

st john’s wort - Paroxetin, Sertraline, Nafazodone

Reduced efficacy due to reduce dopamine level

Kava - Levodopa

Hallucination, psychosis

ginseng - phenelzine

Opposing effect – decreased efficacy

Leafy green veggies rich in vitamin K - Warfarin

Potentiates anticoagulant property

Cranberry juice - warfarin

Enzyme inhibition. Blood levels of the drug increase

grapefruit juice - many drugs

ability of any substance to cause congenital malformations or birth defects

teratogenicity

causes neural tube defects

Carbamazepine & Valproic acid

increased risk of developing vaginal adenocarcinoma syndrome

Diethylstilbestrol

causes Fetal Hydantoin Syndrome

Phenytoin

causes 8th nerve damage

Streptomycin

causes discoloration & defects of teeth & altered bone growth

Tetracyclines

causes Phocomelia

Thalidomide

POWERFUL TERATOGEN

ISOTRETINOIN

unusual reactions that result from termination or sudden discontinuation of the drug (withdrawal syndromes) • uncommon

Type E Reaction (End of Use)

• withdrawal symptoms • generally occur shortly after stopping the drug

Type E Reaction (End of Use)

rebound insomnia & excitation

Benzodiazepine withdrawal

rebound hypertension

Clonidine withdrawal

rebound decongestant

Nasal decongestant withdrawal

adrenal crisis (Addison’s disease)

Steroids withdrawal

▪ unexpected failure of efficacy ▪ common ▪ dose-related

TYPE F REACTIONS (Failure of Efficacy)

Type F reactions may result from:

􏰀 drug-drug interactions 􏰀 use of counterfeit drugs 􏰀 drug instability 􏰀 patient’s non-compliance 􏰀 wrong route of administration 􏰀 drug resistance

Drug Classes that cause the greatest incidence of ADRs

• Antibiotics • Narcotic analgesics • Anticonvulsant • Sedatives • Anticoagulants • Psychotherapeutic drugs • Cardiovascular drugs

Risk Factors for ADR’s

• Age • Associated diseases • Classification of medication being administered • Number of concurrent medications being taken

an injury resulting from medical intervention related to a drug and includes ADRs, but also includes preventable reactions, including those caused by human error

adverse drug event

a response to a drug that is noxious and unintended, and that occurs at doses normally used in humans for the prophylaxis, diagnosis or therapy of disease or for the modification of physiological function

adverse drug reactions

• reactions which occur or arise from the known pharmacological action of a drug in the usual therapeutic doses. • common • predictable • dose-related

TYPE A REACTIONS (Augmented)

related to pharmacological activity of the drug.

Extension Effects

unrelated to pharmacological activity of the drug

Side Effects –

• totally abnormal effects and unrelated to the known therapeutic or pharmacologic actions of a drug. • Uncommon • unpredictable • not dose-dependent • have no relation to the pharmacological action of the drug.

TYPE B REACTIONS (Bizarre)

genetically-determined reactions

Idiosyncrasy

Immune responses to environmental antigens resulting in symptomatic reactions upon secondary exposure to the same antigen, more commonly referred to as allergen.

Hypersensitivity Reactions

• most common category of allergic reaction • occurs after antigen (e.g. pollen) binds onto IgE found on the surfaces of mast cells

Type I (Immediate or Anaphylactic Immune Response)

re-exposure to the same allergen cross linking of the cell-bound IgE degranulation (release of histamines, leukotrienes & prostaglandin

Type I (Immediate or Anaphylactic Immune Response)

initiated by antibody (IgG or IgM) directed against antigens found on the cell membrane of a given target cell (e.g. leukocytes, erythrocytes) complement mediated lysis

Type II (Cytotoxic Reactions)

tissue deposition of antigen-antibody complexes with complement activation and tissue damage

Type III (Immune Complex Hypersensitivity)

▪ T-lymphocytes sensitized by an antigen release lymphokines after subsequent contact with the same antigen ▪ lymphokines induce inflammation and activate macrophages

Type IV (Cell-Mediated or Delayed Type)

• uncommon • long-term effects, dose- & time-related & duration of treatment • associated with the cumulative dose of the drug

TYPE C REACTIONS (Continuous)

Condition where a person takes a drug compulsively, despite potential harm to themselves, or their desire to stop.

Addiction

compulsion to take the drug repeatedly & experiences unpleasant symptoms if discontinued.

Dependence

occurs when a drug has been used habitually & the mind has become emotionally reliant on its effects, either to elicit pleasure or relieve pain and does not feel capable of functioning without it.

Psychological dependence

reduced effect with repeated use of drug; need for higher doses to produce the same effect.

tolerance

􏰀 reactions are manifested long after drug exposure

TYPE D REACTIONS (Delayed)

__ of adults are allergic to one or more medications

__ of ADR’s result from a drug allergy

6-10%

__ of hospital admission are due to ADR’s

__ of ADR’s are preventable

28%

Drug associated with ADR’s: %

29% Analgesics 10% Sedative 9% Antibiotics 7% Antipsychotic.

final Flashcards

(90 cards)