final Flashcards
1+1=0
antagonism
When a drug inhibits or counters or offsets the effect of another drug.
antagonism
When 2 drugs combine in solution so that the effect of the active drug is lost
Chemical antagonism – Neutralization
Type of chemical antagonism where the result is a reduction of the concentration of the active drug at its site of action
Pharmacokinetic antagonism
Object drug (agonist) competes with the precipitant drug (antagonist) for the same receptor.
Pharmacologic: Competitive antagonism
antagonist activity is reduced or cancelled when the agonist concentration is increased.
Reversible competitive antagonism
the action of the antagonist is reversed by increasing the agonist concentration.
The antagonist dissociates very slowly from the receptor.
Irreversible antagonism
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
When the action of the precipitant drug offsets the action of the object drug.
Physiological antagonism
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
Phenobarbital induces metabolism of warfarin resulting in the reduction of plasma concentration of warfarin and reduced anticoagulant.
Pharmacokinetic antagonism
Dimercaprol chelating with heavy metals and thus reduce their toxicity
Chemical antagonism – Neutralization
Caffeine offsetting effect of depressants
Physiological antagonism
Histamine stimulates GI acid secretion while omeprazole inhibits proton pump resulting in reduced acid secretion
Physiological antagonism
Thiazide diuretics elevate blood glucose offsetting the effect of oral hypoglycemic drugs
Physiological antagonism
Depressants counteracting effect of stimulants.
Physiological antagonism
Caffeine Object Drugs
CNS Depressant
Aspirin
Theophylline
Ciprofloxacin
Cimetidine
Oral contraceptives
Prednisone
Milk, Dairy products, Multivitaminsc Antacids, Food containing Ca, Mg, Al Object Drugs
Tetracycline
Bisacodyl
Leafy green veggies – rich in vitamin K and Cranberry juice Object Drug
Warfarin
Theobromine object drug
CNS Depressants
Grapefruit juice object drugs
Many drugs
Tyramine-rich food • Cheese, Red wine object drug
MAO Inhibitors
Histamine – rich food object drugs
Isoniazid, MAOI
Protein – rich food object drugs
Propanolol
Carbidopa/levodopa and theophylline
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
5%
__ of ADR’s result from a drug allergy
6-10%
__ of hospital admission are due to ADR’s
3%
__ of ADR’s are preventable
28%
Drug associated with ADR’s: %
29% Analgesics
10% Sedative
9% Antibiotics
7% Antipsychotic.