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98 Cards in this Set

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Define Tolerance
response diminishes with time
What is Pharmacokinetic tolerance due to?
induction of drug metabolizing enzymes
Alternate names for Pharmacokinetic tolerance
Metabolic tolerance

Drug disposition tolerance
Give an example of Pharmacokinetic Tolerance
Warfarin, an oral anticoagulant, dose needs to be increased in a patient taking barbiturates or Phenytoin
Explain Pharmacodynamic tolerance
-develops at the cellular level

-is due to changes in receptor numbers or function
List the 2 mechanisms of Pharmacodynamic tolerance

Explain Desensitization
process occurs rapidly when continuous exposure to an agonist results in 1) conversion of a channel to an altered state that remains closed or 2) when a receptor-coupling element is phosphorylated to an inactive form
What cause receptor down-regulation
Explain Down-regulation
process of ligand-induced endocytosis and degradation of receptor, caused by agonists when administered at high doses for a prolonged period
Give 3 examples of Pharmacodynamic Tolerance
1. continuous exposure to beta-adrenergic agonists,such as occurs in treatment of asthma with ALBUTEROL, results in a decreased responsiveness to the drug

2. tolerance to the analgesic effects of MORPHINE upon continued use

3. decreased sedation from continuous treatment with a Benzodiazepine such as DIAZEPAM
Explain Physiological Antagonism
when 2 agents have opposing physiological effects
Give an example of Physiological antagonism
Histamine causes Vasodilation while NE causes Vasoconstriction -> when given together they counteract eachother
Explain Competitive Antagonism
when a receptor antagonist is administered with an agonist
Competitive Antagonism: what does Naloxone block the effect of?
Competitive Antagonism: what does Atropine block the effect of?
ACh at muscarinic receptor
Competitive Antagonism: what does Propranolol block the effect of?
Isoproterenol at beta-adrenergic receptors
Describe how Supersensitivity or Hyperactivity occurs
due to an increase in the number of receptors
-during absence of ligand
-prolonged presence of antagonist
Give an example of Chemically induced supersensitivity
after prolonged treatment with Beta-blockers some individuals become supersensitive to endogenous release of Catecholamines (Epi, NE, Dopa)
Explain Denervation induced Supersensitivity
occurs at POST-synaptic receptors when Pre-synaptic nerve is surgically destroyed or lesioned
What causes receptor up-regulation?
Pharmacogenetic cause of increased activity of drugs
deficiency in degrading enzymes
Patients with abnormal serum cholinesterase have increased sensitivity to what drug?
Succinylcholine = muscle relaxant
Individuals with Glucose-6-phosphate Dehydrogenase deficiency develop Acute Hemolytic Anemia after given what drug?
Explain how competition for binding sites can result in increased activity of a drug
drugs may displace one another from plasma albumin binding sites, enhancing response to one or both agents
T or F: If a drug is displaced from a plasma protein-binding site, response is INTENSIFIED and duration of action is PROLONGED
False: duration is shortened
Explain how Physiological Synergism can increase activitiy of drugs
when 2 drugs produce the same or similar effects through different receptors or mechanisms
Explain an additive effect
when two drugs are given and their effect is like adding their individual effects together

5+5 = 10
Classic Example of 2 drugs that act synergistically
Diazepam + Ethanol produce severe, prolonged CNS depression
Explain Synergistic effect
When two drugs are added together and their effects together are greater than when adding their effects alone

5 + 5 = 15
Explain Potentiation
one drug might not have an effect alone but in combo with other drugs it
has an effect

0+5 = 20
Definition: repeated administration produces altered or adaptive physiological state and physiological disturbances (withdrawal, abstinence syndrome) occur if drug is not present
Physical Dependence
Drugs that result in dependence (4)
1. Alcohol
2. Barbiturates
3. Narcotic analgesics
4. Nicotine
Definition: Compulsive drug-seeking behavior; individual uses drug repetitively for personal satisfaction
Psychological dependence
Definition: cluster of symptoms indicating that the individual continues substance use despite significant substance-related problems
Substance dependence (addiction)
Overextension of Pharmacological response: Atropine induces _______
Dry mouth
Overextension of Pharmacological response: Propranolol induced _______
Heart Block
Overextension of Pharmacological response: Diazepam-induced _______
Organ-directed toxicities: Aspirin-induced _______
GI toxicity
Organ-directed toxicities: Aminoglycoside-induced ______
Renal toxicity
Organ-directed toxicities: Acetaminophen-induced ______
Organ-directed toxicities: Doxorubicin-induced ______
Cardiac toxicity
Direct fetal toxic effects: Sulfonamide-induced ______
Kernicterus = damage to the brain centers of infants caused by jaundice
Direct fetal toxic effects: Chloramphenicol-induced ________
Gray baby syndrome
Direct fetal toxic effects: Tetracycline-induced _______
-teeth discoloration

-Retardation of bone growth
When are Teratogenic effects most pronounced?
during organogenesis: day 20 - end of 1st trimester
List 8 human teratogens
1. Thalidomide
2. Antifolates
3. Phenytoin
4. Warfarin
5. Isotretinoin
6. Lithium
7. Valproic acid
8. Fetal alcohol syndrome
VALerie is an ANTIFOLATE from THAILAND. Her country is at WAR with the PHENYTOIN's. They give their babies LITHIUM AND ISOTRETINOIN which yields FETAL ALCOHOL SYNDROME
Definition: Abnormal response resulting from previous sensitizing exposure activating immunologic mechanism
Drug allergies (hypersensitivity)
T or F: in drug allergies, altered reaction occurs only in a fraction of the population
T or F: In drug allergies the dose-response is unusual: a large amount of an otherwise safe drug elicits severe reaction
False: minute amounts elicit a severe reaction
T or F: In drug allergies the manifestations of reaction are similar to the pharmacological and toxicological effects of the drug
False: they are different
T or F: Drug allergies
-Primary sensitization period occurs before the individual experiences the response
T or F: Drug allergies
-Most drug by themself are immunogenic
False: Being small molecules, most drugs by themselves are not immunogenic; they bind covalently to self-macromolecule or alter structure of self-macromolecule to become immunogenic
Fill in the table
Explain the Type I Hypersensitivity reaction
-IgE molecules bind to blood basophils and tissue mast cells via Fc receptors for antibody
-When offending drug introduced into body, immediately binds to IgE bound to sensitized cells, resulting in release of mediators (histamine, leukotrienes, prostaglandins)
-Mediators initiate skin and smooth muscle responses, cause tissue injury and provoke inflammatory response
-Include anaphylaxis, urticaria and angioedema
Explain Type II Hypersensitivity reactions
mediated by IgM or IgG binding to cells or tissues, resulting in the activation of complement and lysis of the cell
Explain Type III Hypersensitivity reactions
mediated by Immune complexes
What are symptoms of Immune-complex induced serum sickness?
-Urticarial skin eruptions
What is the name of the severe form of immune vasculitis caused by drugs?

What drug can induce it?
Stevens-Johnson syndrome

Explain Type IV Hypersensitivity reaction
cell-mediated or delayed hypersensitivity, often occurs when drugs are applied topically
Type II reactions: Penicillin-induced _________
hemolytic anemia
Type II reactions: Methyldopa-induced __________
autoimmune hemolytic anemia
Type II reactions: Quinidine-induced _______
Type II reactions: Sulfonamide-induced ________
5 drugs that can induce Type III Immune Vasculitis

Definition: Abnormal response not immunologically mediated; often caused by genetic abnormalities in enzymes or receptors; referred to as pharmacogenetic disorders.
Drug Idiosyncrasies
Classical idiosyncracy: patients with abnormal serum Cholinesterase develop _____ when given normal doses of succinylcholine
Apnea = temporary suspension in breathing
"Slow" acetylators of Isoniazid are homozygous autosomal recessive for this gene's protein
What are "slow" acetylators of isoniazid more prone to?
isoniazid-induced Vitamin B6 deficiency which may produce:
-various neuropathies

**Supplement with B6 when treating TB with Isoniazid
Hemolytic anemia in patients with G-6-P Dehydrogenase can be induced by these 3 drugs
1. Primaquine
2. Sulfonamides
3. Nitrofurantoin
_______-induced Porphyria occurs in individuals with abnormal ______ biosynthesis

Explain how Barbiturates can induce Porphyria
-the Barbiturate acid moeity mimics part of the Heme structure, occupying a portion of the heme site on the protein that regulates production of ALA synthetase
-Heme is a repressor, inhibiting production of ALA synthetase and reducing porphyrin production
= without Heme present inhibiting the production of ALA synthetase, Porphyrin production will increase
Definition: Application of the principles of pharmacokinetics, pharmacodynamics and adverse effects to the treatment of patients
The incidence of a placebo response is constant between what percents in clinical trials?
20 and 40%
Drug whose resin binds with other drugs and prevents their
Antacids have metals that chelate with these 2 drugs and prevent their absorption

Group of drugs that decrease GI motility and slow absorption of many drugs
Anticholinergics (Atropine)
GI motility alteration may alter absorption of some of this group of drugs
Weak organic acids
3 groups of plasma protein binding drugs that can displace drugs from albumin
1. Oral hypoglycemic agents (tolbutamide)
2. Oral anticoagulants (warfarin)
3. Antimetabolites (methotrexate)
Digoxin can be displaced from its tissue binding sites by this drug
Alkalinization of urine (Sodium Bicarb) enhances excretion of ________
Weak organic acids
Acidification (ammonium chloride) of urine enhances the excretion of _______
weak organic bases
What drug blocks the tubular excretion of penicillin?
Administration of these two nephrotoxic drugs can produce kidney damage even when dose of either agent alone may have been insufficient to produce toxicity

What 2 properties of drugs are regulated by the FDA?

What is filed with the FDA once a potential drug is judged ready to be initiated for Human studies
Investigational New Drug (IND) exemption
What is the goal in Phase 1 of Human Testing?
to find the maximum tolerated dose = "Is it safe?"
What is always the first dose in Phase 1 human testing?
T or F: testing is never double-blind in Phase 1 testing
What is the definition of Phase 2 human testing?
first attempt to determine clinical effectiveness of test agent = "Does it work?"
T or F: Phase 2 tests may be single-blind or double-blind and involve hundreds of patients
What is the definition of Phase 3 human testing?
extensive testing of a drug's efficacy and toxicity = "How well does it work, and what are the common side effects?"
Phase 1 and 2 studies are usually conducted by __1__, but Phase 3 may include __2__
1. Clinical scientists

2. physicians in private practice
After completion of Phase 3 testing, company files _________with the FDA
New Drug Application
Fewer than how many subjects are usually tested before Phase 4?
What is Phase 4 human testing?
post-marketing surveillance = when adverse effects and toxicity become most evident
During which Phases is informed consent required?
Phase 1-3
Informed consent must be in writing for which Phases?
1 and 2
Who protects the interest of the subjects in Phase testing?
Peer review (Committee on Human Experimentation)