PHARM BASICS Flashcards
Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
Plasma concentration of a drug at a given time
Cp
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of unchanged drug that reaches systemic circulation after administration
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
Different steps of Phase I
Oxidation, reduction, hydrolysis
Barbiturates, phenytoin, carbamazepine, and rifampin all do this
Induce CYP450
Cimetidine, ketoconazole, isoniazid, and grapefruit all do this
Inhibit CYP450
Name 3 Phase II conjugation reactions
Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation
Constant percentage of drug metabolized per unit time
First order kinetics
Constant amount of drug metabolized per unit time
Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect compared with another drug
Potency
Ability of drug to produce the maximal biologic effect
Efficacy
Ability of a drug to produce maximal response after binding to the receptor
Full agonist
Ability to produce less than maximal response after binding to the receptor
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site
Noncompetitive antagonist
Mechanism of action (MOA) utilizes intracellular receptors
Steroid and hormones
Mechanism of action (MOA) utilizes transmembrane receptors that have intrinsic enzymatic activity
Insulin, EGF, TGFbeta, PDGF, ANP
Mechanism of action (MOA) utilizes ligand gated ion channels
Acetylcholine, nicotine
Dose which produces therapeutic response in 50% of the population
ED50
Dose which is toxic in 50% of the population
TD50
Dose which is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Drugs that have a high margin of safety is indicated by
High therapeutic index
Drugs that have a narrow margin of safety is indicated by
Low therapeutic index
Antidote used for lead poisoning (without encephalopathy)
Dimercaprol, Edetate calcium disodium, or succimer
Antidote used for cyanide poisoning
Nitrites, sodium thiosulfate, hydroxocobalamin (cyanokit)
Antidote used for anticholinergic poisoning
Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity
Deferoxamine
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine
Antidote for severe lead poisoning (with encephalopathy)
Dimercaprol AND CaEDTA (edetate calcium disodium)
Antidote for arsenic, mercury, and gold poisoning
Dimercaprol
Antidote used in Wilson’s disease (copper poisoning)
Penicillamine
Antidote used for heparin toxicity
Protamine Sulfate
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol toxicity
Ethanol
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
Antidote for methotrexate toxicity
Leucovorin
Antidote for beta-blocker overdose and hypoglycemia
Glucagon
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate)
Method to reduce salicylate intoxication
Alkalinize urine, dialysis