HB-1 Exam 2 flashcards-Week 3 Gems.txt

activates glucocorticoid receptor, alters transcription of various enzymes

Serine

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

Methanol-->formate (via alcohol dehydrogenage)--> toxic metabolites. IV ethanol has greater affinity for ADH and blocks methanol metabolism.

effect of the body on the drug (ADME)

effect of a drug on the body at the molecular level

the use of drugs to diagnose, prevent or treat disease, or prevent pregnancy

Effective dose-the concentration at which 50% of pts show a defined response

the ability of a drug to produce a maximal response

Refers to the amount of drug necessary to elicit a desired response?

describes the diminished physiologic response to a drug after repeated administration of a constant does (aka tachyphylaxis and desensitization)

Aspirin-Hippocrates (400BC) and Johann Buchner (1829)--Bayer(1899)

1st law concerning drug safety and efficacy. required accurate labeling of ingredients and sought to prevent adulteration of products with toxic or inactive ingredients

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

Created a legal distinction between prescription and non-prescription drugs

required demonstration of drug safety and efficacy in animals and humans prior to drug marketing-established phases 1-IV of clinical trials

sought to encourage drug development of agents for rare diseases

accelerated approval time for generic drug products (instead of NDA, submit ANDA) which are demonstrated to be bioequivalent

driven by AIDS and cancer epidemics. allow pts with said diseases to be treated with investigational drugs prior to completion of clinical trials

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

Aims to determine if repeated doses affect fertility, implantation, fetal growth, generation of fetal abnormalities and neonatal growth

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

to determine the pharmacokinetic parameters of the drug in healthy volunteers, also evaluate toxicity by liver and renal function

to determine the pharmacology of the drug in patients with the intended clinical condition-determine min and max dose

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

To monitor drug safety in the general pt population following FDA approval, post-marketing surveillance (Pharmacovigilance)

generic

dietary supplements-legally distinct from prescription and OTC meds-don't need to demonstrate safety and efficacy prior to marketing

claims to be anxiolytic and induce relaxation; linked to hepatotoxicity

Both are effective antimalarial agents; quinidine can be used as an atiarrhythmic

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

Kd: when 50% of receptors are bound. Bmax: 100% of receptors bound

The concentration of drug that produces 50% maximal effect.

beta lactam antibiotics-penicillins and cephalosporins, NSAIDs, ASA

Local anesthetics, opiod analgesics, sedative/hypnotics, anti-emetics, antipsychotics, antidepressants, Lidocaine, Propanolol

alpha1acid glycoprotein binds basic drugs, albumin binds acidic drugs.

increased polarity and smaller Vd.