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Z - Pharmacology

First Aid - Pharm 2

QuestionAnswer
Formula for maintenance dose Cp * CL / F ;;Cp = target plasma concentration F = bioavailibility
In patients with impaired renal or hepatic function, the loading dose decreases, increases or remains unchanged? Maintenance dose? Loading dose remains unchanged Maintenance dose decreases
Rate of elimination is constant (constant amount of drug is eliminated per unit time) - what order elimination? What happens to target plasma concentration? Zero order elimination Target plasma concentration decreases linearly with time
Rate of elimination is proportional to drug concentration (constant fraction of drug eliminated per unit time) - what order elimination? What happens to target plasma concentration? First order elimination Cp decreases exponentially with time
Give examples of drugs with zero order elimination Ethanol Phenytoin Aspirin (at high or toxic concentration)
Phase I metabolism ;products, what happens and how eliminated (reduction, oxidation, hydrolysis) yields _ slightly polar, water-soluble metabolites (often still active) not yet eliminated
What phase of metabolism associated with cytochrome P450 Phase I
What phase of metabolism associated with conjugation Phase II
Phase II metabolism ;products, what happens and how eliminated acetylation, glucoronidation, sulfation) yields Very polar, inactive metanolites (renally excreted)
Geriatric patients lose which phase of metabolism first? Phase I
Is it safe? Pharmacokinetics? - which phase of clinical testing of the drug Phase I
Does it work in patients?- which phase of clinical testing of the drug Phase II
Does it work? Double blind - which phase of clinical testing of the drug Phase III
What happens in phase IV of clinical testing of the drug Postmarketing surveillance
A competitive antagonist shifts agonist curve where? To the right
A noncompetitive antagonist (irreversible) shifts agonist curve where? Downward
Urine pH and drug elimination;;what is trapped Ionized species get trapped.
Urine pH and drug elimination;;Ionized species Ionized species get trapped.
Urine pH and drug elimination;;Weak acids what and Tx Trapped in basic environments. Treat overdose with bicarbonate.
Urine pH and drug elimination;;Weak bases what and Tx Trapped in acidic environments. Treat overdose with ;ammonium chloride.
Urine pH and drug elimination;;Trapped in basic environments. Weak acids
Urine pH and drug elimination;;Trapped in acidic environments. Weak bases
dose response curves and;;different antagonists A. A competitive antagonist shifts curve to the right, decreasing potency and ↑ EC50.;;B. A noncompetitive antago-;nist shifts the agonist curve downward, decreasing efficacy.
dose response curves and;;shifts curve to the right, decreasing potency and ↑ EC50. competitive antagonist
dose response curves and;;shifts the curve downward, decreasing efficacy. noncompetitive antago-;nist
dose response curves and;;in a system with spare receptors the EC50 is lower than the Kd, indicating that to achieve 50% of maximum effect, < 50% of the receptors must be activated. EC50: dose causing 50% of maximal effect. Kd: concentration ofdrug required to bind 50% of receptor sites.
dose response curves and;;different agonists 1. The partial agonist acts on the same receptor system as the full agonist but has a lower maximal efficacy no matter the dose. ;;A partial agonist;may be more potent (as in the figure), less potent, or equally potent; potency is an independent factor.
dose response curves and;;may be more potent (as in the figure), less potent, or equally potent; potency is an independent factor. A partial agonist
Efficacy maximal EFFECT
Potency amount needed for a given EFFECT
amount needed for a given EFFECT Potency
maximal EFFECT Efficacy
Therapeutic index TILE;;LD50/ED50
pre and postsynaptic nervous system neurotransmitters;;Parasymp ACh;(nicotinic);;ACh;(muscarinic)
pre and postsynaptic nervous system neurotransmitters;;Somatic only one ;ACh (nicotinic)
pre and postsynaptic nervous system neurotransmitters;;Sympathetic pre = ACh (nicotinic);;Ach (muscarinic)- sweat glands ;;NEα,β - Cardiac and smooth;muscle, gland cells, ;nerve terminals;;D1 - Renal vascular smooth muscle
nicotinic receptor mech ACh ligand gated Na+/K+ channels
muscarinic receptor mech ACh G- protein coupled receptors that act through 2nd messengers
ACh ligand gated Na+/K+ channels nicotinic receptor
ACh G- protein coupled receptors that act through 2nd messengers muscarinic receptor
G-protein-linked 2nd messengers ;give G protein and major function;;α1 Receptor q ;;↑ vascular smooth muscle contraction
G-protein-linked 2nd messengers ;give G protein and major function;;α2 Receptor i ;;↓ sympathetic outflow, ↓ insulin release
G-protein-linked 2nd messengers ;give G protein and major function;;β1 Receptor s ;;↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous ;humor formation
G-protein-linked 2nd messengers ;give G protein and major function;;β2 Receptor s ;;Vasodilation, bronchodilation, ↑ glucagon release
G-protein-linked 2nd messengers ;give G protein and major function;;M1 Receptor q ;;CNS
G-protein-linked 2nd messengers ;give G protein and major function;;M2 Receptor i ;;↓ heart rate
G-protein-linked 2nd messengers ;give G protein and major function;;M3 Receptor q ;;↑ exocrine gland secretions
G-protein-linked 2nd messengers ;give G protein and major function;;D1 Receptor s ;;Relaxes renal vascular smooth muscle
G-protein-linked 2nd messengers ;give G protein and major function;;D2 Receptor i ;;Modulates transmitter release, especially in brain
G-protein-linked 2nd messengers ;give G protein and major function;;H1 Receptor q ;;↑ nasal and bronchial mucus production, contraction of bronchioles,pruritus, and pain
G-protein-linked 2nd messengers ;give G protein and major function;;H2 Receptor s ;;↑ gastric acid secretion
G-protein-linked 2nd messengers ;give G protein and major function;;V1 Receptor q ;;↑ vascular smooth muscle contraction
G-protein-linked 2nd messengers ;give G protein and major function;;V2 Receptor s ;;↑ H2O permeability and reabsorption in the collecting tubules of ;the kidney
Given the major function and G-protein class name the receptor;;q ;↑ vascular smooth muscle contraction α1
Given the major function and G-protein class name the receptor;;i ;↓ sympathetic outflow, ↓ insulin release α2
Given the major function and G-protein class name the receptor;;s ;↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous ;humor formation β1
Given the major function and G-protein class name the receptor;;s ;Vasodilation, bronchodilation, ↑ glucagon release β2
Given the major function and G-protein class name the receptor;;q ;CNS M1
Given the major function and G-protein class name the receptor;;i;↓ heart rate M2
Given the major function and G-protein class name the receptor;;q ;↑ exocrine gland secretions M3
Given the major function and G-protein class name the receptor;;s ;Relaxes renal vascular smooth muscle D1
Given the major function and G-protein class name the receptor;;i ;Modulates transmitter release, especially in brain D2
Given the major function and G-protein class name the receptor;;q ;↑ nasal and bronchial mucus production, contraction of bronchioles, H1
Given the major function and G-protein class name the receptor;;s ;↑ gastric acid secretion H2
Given the major function and G-protein class name the receptor;;q ;↑ vascular smooth muscle contraction V1
Given the major function and G-protein class name the receptor;;s ;↑ H2O permeability and reabsorption in the collecting tubules of the kidney V2
G-protein-linked 2nd messengers ;Receptor G-protein class ;;how to remember which goes with which α1, α2, β1, β2, M1, M2, M3, D1, D2, H1, H2, V1, V2;;"QISS (kiss) and QIQ (kick) till you're SIQ (sick) of SQS (sex)."
G-protein-linked 2nd messengers ;Receptor G-protein class ;;3rd messengers... for Gq HAVe 1 M&M (H1, α1, V1, M1, M3);;↑ Phospholipase C to IP3 (↑Ca2+) and DAG (Protein Kinase C)
G-protein-linked 2nd messengers ;Receptor G-protein class ;;3rd messengers... for Gs β1, β2, D1 H2, V2 ;;↑ Adenylcyclase (↑ATP to cAMP [ ↑ Protein kinase A])
G-protein-linked 2nd messengers ;Receptor G-protein class ;;3rd messengers for... Gi MAD 2's (M2, α2, D2);;↓Adenylcyclase (↓ATP to cAMP [ ↑ Protein kinase A])
Release of NE from a sympathetic nerve ending is modulated by;;with mech by NE itself, acting on presynaptic α2 autoreceptors, and by ACh, ;;angiotensin II, and other substances.
Created by: christinapham