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86 Cards in this Set

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  • Back
What do pharmacokinetics describe?
Where the drug goes and how much needed for desired effect.
What factors affect pharmacokinetics?
Absorption, distribution, metabolism, and excretion.
What affects absorption?
Rate is affected by route of drug administration and extent is determined by metabolism and lipid solubility.
What affects the distribution?
Diffusion across gradient, lipid/water partitioning, charge and pH.
Are most drugs weak acids or weak bases?
Are drugs more likely to be trapped in ionized or neutral form?
Ionized, since ions don't easily cross membranes.
How is the metabolism of a drug defined?
Clearance from the body compartments and eventual elimination from the body.
What is first pass metabolism?
The reduction in bioavailability in orally administered drugs.
What is the volume of distribution (Vd) and what are the units?
Vd = dose/plasma concentration (liters/kg)
What has a higher Vd, protein-bound drugs or lipid soluble drugs?
Lipid soluble drugs have a much higher Vd.
What is clearance (CL)?
(CL = ke * Vd) or the ratio of the rate of elimination by all routes to the concentration of drug in biological fluids.
Where does most elimination (ke) occur?
Through the liver and kidney, and is usually either 1st or 0th order.
What is the half-life of a drug?
half-life = 0.693 * Vd/CL
What is the dosing rate at steady state (DRss)?
DRss = CL * TC/F , where F=bioavailability fraction. Rule of thumb indicates that it takes 4-5 half lives to reach the steady state level.
How do you calculate the maintenance dose (MD)?
MD = DR/F * DI, where DI = dosing interval
What is the loading dose (LD)?
LD = Vd * TC, where TC = target concentration.
What are pharmacodynamics?
This term describes how a drug works. This is determined by 1) drug-receptor interactions; 2) duration of drug action.
What are the 2 phases in drug metabolism?
Phase I = conversion of drug to more polar or reactive compound; Phase II = increase water solubility to increase water solubility.
What are the cytochrome P-450 group of enzymes?
Enzymes located in the smooth ER which help catabolize drugs.
What is the effect of CIMETIDINE?
CIMETIDINE is a P-450 inhibitor and slows down drug metabolism.
What is the rule of thumb which tells you whether a drug is a weak acid or a weak base?
The sodium salt of a drug indicates a weak acid and the HCl salt of a drug indicates a weak base.
What is an alkanizing agent?
What is and acidifying agent?
ammonium chloride
What are some factors that affect Vd?
disease (obesity, renal disease), size (capillary permeability), lipid solubility, and charge
What does it mean when the rate of elimination is a first order event?
The ke is dependent on concentration and elimination is not saturable.
What does zero order elimination rate meatn?
The ke is independent of concentration, elimination IS saturable, and half-life is unpredictable.
What are examples of drugs with a zero order elimination rate?
aspirin, alcohol, and phenytoin
What proportion of the therapeutic level of a drug is remaining after 3 half-lives of dosing?
87.5% (1 hl = 50%, 2 hl = 75%)
What are the 3 basic reactions in Phase I of drug metabolism?
oxidation, reduction, and hydrolysis
P-450 is responsible for which Phase I reaction?
What are 4 reactions in Phase II drug metabolism?
glucoronidation, sulfation, acetylation and glutathione conjugation
Which is the most important organ in drug metabolism?
Liver is most important, followed by the kidney.
What are the 2 components of the cytochrome P-450 enzyme system?
oxidase and reductase
What are examples of P-450 inducers?
barbiturates, ethanol, which enhance the metabolism of warfarin (anticoagulant) and tylenol (analgesic), respectively.
What are examples of P-450 inhibitors?
cimetidine and allopurinol, which decrease the metabolism of valium and tolbutamide, respectively
What is the EC50?
Concentration of a drug required to yield 50% of maximal effect.
What drugs act through competitive antagonism?
propranolol and atropine
What drug acts as a non-competitive antagonist?
Which drugs are full agonists?
norepinephrine and acetylcholine
Which drug is a partial agonist?
What two neuronal receptors are coupled to ion channels?
Cholinergic nicotinic receptors and GABA receptors.
Which two neuronal receptors are coupled to adenyl cyclase?
beta-adrenoreceptors and alpha2-adrenoreceptors
Which two neuronal receptors are coupled to diacylglycerol and inositol triphosphate?
alpha1-adrenoreceptors and cholinergic muscarinic receptors.
What are the 6 steps associated with neurotransmission in a cholinergic neuron?
synthesis, storage, release, binding, degradation, choline recycling
What is the name of the enzyme that catalyzes combination of acetyl CoA with choline to form Ach in the cytosol?
choline acetyltransferase (CAT).
What is the effect of botulinum toxin?
Blocks the release of the Ach-filled vesicles at the pre-synaptic terminal.
What is the function of acetylcholinesterase?
Cleaves Ach to acetylcholine and choline.
Name 4 direct-acting cholinergic agonists.
acetylcholine, bethanechol, carbachol, pilocarpine
Name 4 indirect acting, reversible, cholinergic agonists.
edrophonium, neostigmine, physostigmine, pyridostigmine.
What are 2 indirect-acting, irreversible, cholinergic agonists.
echothiophate, isofluorophate.
How many different types of muscarinic receptors are there?
5: M1-M5.
Where are M1 receptors located?
Gastric parietal cells.
Where are M2 receptors located?
Cardiac cells and smooth muscle.
Where are M3 receptors located?
Exocrine glands and smooth muscle.
What is the mechanism of action of the M2 subtype muscarinic receptor?
G protein stimulation, AC inhibition, increased K+ conductance, decreased rate and force of contraction.
Effects of a1 stimulation.
vasoconstriction, + peripheral resistance, + BP, mydriasis, + closure of internal sphincter of bladder
Effects of a2 stimulation.
inhibit NE release, inhibit insulin release
Effects of b1 stimulation.
tachycardia, + lipolysis, + myocardial contractility
Effects of b2 stimulation.
vasodilation, slight - in peripheral resistance, bronchodilation, + liver & muscle glycogenolysis, + glucagon release, relaxed uterine smooth muscle
What are the 5 catecholamines used widely clinically?
DINED - dopamine, isoproterenol, norepinephrine, epinephrine, dobutamine
What are the target receptors and therapeutic uses of epinephrine?
(a1, a2, b1, b2); acute asthma, open-angle glaucoma, anaphylactic shock, in local anesthetics to + duration of action
What are the target receptors and therapeutic uses of norepinephrine?
(a1, a2, b1); treatment of shock
What are the target receptors and therapeutic uses of isoproterenol?
(b1, b2); bronchodilator in asthma, cardiac stimulant
What are the target receptors and therapeutic uses of dopamine?
(dopaminergic, b1); treatment of shock, congestive heart failure
What are the target receptors and therapeutic uses of dobutamine?
(b1); congestive heart failure
What are the target receptors and therapeutic uses of phenylephrine?
(a1); nasal decongestant, treatment of supraventricular tachycardia
What are the target receptors and therapeutic uses of methoxamine?
(a1); treatment of supraventricular tachycardia
What are the target receptors and therapeutic uses of clonidine?
(a2); hypertension
What are the target receptors and therapeutic uses of metaproterenol?
(b2>b1); treatment of bronchospasm
What are the target receptors and therapeutic uses of terbutaline, ritodrine, and albuterol?
(b2); treatment of bronchospasm and premature labor
What are the target receptors and therapeutic uses of amphetamine?
(a, b, CNS); CNS stimulant in treatment of children with attention deficit syndrome
What are the target receptors and therapeutic uses of ephedrine?
(a, b, CNS); treatment of asthma, nasal decongestant
What is the receptor selectivity and therapeutic use of propranolol?
(b1, b2); hypertension, glaucoma, migraine, hyperthyroidism, angina pectoris, myocardial infarction
Are black and white patients equally responsive to all hypertension treatments?
No, black patients are not as responsive to b-blocker therapy.
Why are b-blockers contraindicated in patients with asthma or COPD?
b2 blockade leads to bronchoconstriction
What is the effect of b-blockers on renal perfusion?
Lower blood pressure leads to decreased renal perfusion, resulting in Na+ retention and + plasma volume.
What is the receptor selectivity and therapeutic use of timolol?
(b1, b2); glaucoma, hypertension
What is the receptor selectivity and therapeutic use of acebutolol, atenolol, metoprolol?
(b1); hypertension
What is the receptor selectivity and therapeutic use of labetalol?
(a1, b1, b2); hypertension
What is commonly used to treat hypertension?
propranolol, metoprolol, timolol, other b-blockers reduce cardiac output and renin secretion
What is commonly used to treat glaucoma?
Timolol, and other b-blockers reduce secretion of aqueous humor.
What is commonly used to treat migraine?
Propranolol provides prophylactic effect.
What is commonly used to treat thyrotoWhat is commonly used to treatosis?
Propranolol reduces cardiac rate and potential for arrhythmias.
What b-blockers are indicated for arrhythmia prophylaWhat is commonly used to treatis after MI?
Propranolol, Metoprolol and timolol reduce CO and renin secretion.
What b-blockers are used for supraventricular tachycardias?
Propranolol, esmolol, and acebutolol slow AV conduction velocity.
What is commonly used to treat angina pectoris?
Propranolol, nadolol, and other b-blockers reduce cardiac rate and force.