activates glucocorticoid receptor, alters transcription of various enzymes
Which is more common: serine or tyrosine kinase?
What is irreversible inhibition?
Inhibitor covalently binds E at the same site as S irreversibly changes E (suicide analogue), can't overcome S, Km doesn't change, Vmax decreases
What is the pathway of methanol metabolism and what can block it?
Methanol-->formate (via alcohol dehydrogenage)--> toxic metabolites. IV ethanol has greater affinity for ADH and blocks methanol metabolism.
What is pharmacokinetics?
effect of the body on the drug (ADME)
What is pharmacodynamics?
effect of a drug on the body at the molecular level
What is therapeutic?
the use of drugs to diagnose, prevent or treat disease, or prevent pregnancy
What is ED50?
Effective dose-the concentration at which 50% of pts show a defined response
What is efficacy?
the ability of a drug to produce a maximal response
What is potency?
Refers to the amount of drug necessary to elicit a desired response?
What is tolerance?
describes the diminished physiologic response to a drug after repeated administration of a constant does (aka tachyphylaxis and desensitization)
What is the first synthetic drug?
Aspirin-Hippocrates (400BC) and Johann Buchner (1829)--Bayer(1899)
What is the Pure Food and Drug Act-1906?
1st law concerning drug safety and efficacy. required accurate labeling of ingredients and sought to prevent adulteration of products with toxic or inactive ingredients
What is Food, Drug, and Cosmetic Act 1938?
required evidence of drug safety before marketing. established FDA, gave legal authority to USP to govern composition of all drugs marketed in US. standards for drug labels
What is the Durham-Humphrey Amendment-1952?
Created a legal distinction between prescription and non-prescription drugs
What is the Kefauver-Harris Amendment-1962?
required demonstration of drug safety and efficacy in animals and humans prior to drug marketing-established phases 1-IV of clinical trials
What is the Orphan Drug Amendment-1983?
sought to encourage drug development of agents for rare diseases
What is the Drug, Price Competition and Patent Restoration Act-1984?
accelerated approval time for generic drug products (instead of NDA, submit ANDA) which are demonstrated to be bioequivalent
What is the accelerated Drug Approval for New Drugs to Treat Life Threatening Conditions-1992?
driven by AIDS and cancer epidemics. allow pts with said diseases to be treated with investigational drugs prior to completion of clinical trials
What is the purpose of preclinical studies?
to establish a pharmacological profile for the agent, pharmicokinestics and toxicological effects--in vitro effects on isolated cells/organs, receptor-binding characteristics, potential therapeutic use
What is teratogenesis?
Aims to determine if repeated doses affect fertility, implantation, fetal growth, generation of fetal abnormalities and neonatal growth
What is an IND?
Investigational New Drug notice-done prior to Phase I studies, gets info on composition and source of drug, manufacturing info, data from animal studies, clinical plans and protocols, names of physicians conducting the trials
What is the goal of Phase I clinical studies?
to determine the pharmacokinetic parameters of the drug in healthy volunteers, also evaluate toxicity by liver and renal function
What is the goal of Phase II clinical studies?
to determine the pharmacology of the drug in patients with the intended clinical condition-determine min and max dose
What is the goal of Phase III clinical studies?
To compare the safety and efficacy of the IND with that of another substance or treatment approach, use placebo-controlled studies, double blinding, cross-over studies
What is the goal of Phase IV clinical studies?
To monitor drug safety in the general pt population following FDA approval, post-marketing surveillance (Pharmacovigilance)
What is the name we go by universally for drugs?
What are nutriceuticals?
dietary supplements-legally distinct from prescription and OTC meds-don't need to demonstrate safety and efficacy prior to marketing
What is kava kava?
claims to be anxiolytic and induce relaxation; linked to hepatotoxicity
What is the difference between Quinidine and quinine?
Both are effective antimalarial agents; quinidine can be used as an atiarrhythmic
What is nortriptyline?
antidepressent-acts by blocking NE uptake transportes on noradrenergic neurons in the CNS---side effect: can cause CV effects by clocking alpha 1 adrenergic on vascular smooth m
What is Kd? What is Bmax?
Kd: when 50% of receptors are bound. Bmax: 100% of receptors bound
What is EC50?
The concentration of drug that produces 50% maximal effect.
What are the acidic drugs?
beta lactam antibiotics-penicillins and cephalosporins, NSAIDs, ASA
What are the basic drugs?
Local anesthetics, opiod analgesics, sedative/hypnotics, anti-emetics, antipsychotics, antidepressants, Lidocaine, Propanolol
What binding protein binds acidic drugs? basic?
alpha1acid glycoprotein binds basic drugs, albumin binds acidic drugs.