First Aid - Pharm 2
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| Formula for maintenance dose | Cp * CL / F ;;Cp = target plasma concentration F = bioavailibility
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| 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
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| 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
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| 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
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| Give examples of drugs with zero order elimination | Ethanol Phenytoin Aspirin (at high or toxic concentration)
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| Phase I metabolism ;products, what happens and how eliminated | (reduction, oxidation, hydrolysis) yields _ slightly polar, water-soluble metabolites (often still active) not yet eliminated
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| What phase of metabolism associated with cytochrome P450 | Phase I
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| What phase of metabolism associated with conjugation | Phase II
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| Phase II metabolism ;products, what happens and how eliminated | acetylation, glucoronidation, sulfation) yields Very polar, inactive metanolites (renally excreted)
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| Geriatric patients lose which phase of metabolism first? | Phase I
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| Is it safe? Pharmacokinetics? - which phase of clinical testing of the drug | Phase I
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| Does it work in patients?- which phase of clinical testing of the drug | Phase II
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| Does it work? Double blind - which phase of clinical testing of the drug | Phase III
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| What happens in phase IV of clinical testing of the drug | Postmarketing surveillance
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| A competitive antagonist shifts agonist curve where? | To the right
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| A noncompetitive antagonist (irreversible) shifts agonist curve where? | Downward
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| Urine pH and drug elimination;;what is trapped | Ionized species get trapped.
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| Urine pH and drug elimination;;Ionized species | Ionized species get trapped.
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| Urine pH and drug elimination;;Weak acids what and Tx | Trapped in basic environments. Treat overdose with bicarbonate.
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| Urine pH and drug elimination;;Weak bases what and Tx | Trapped in acidic environments. Treat overdose with ;ammonium chloride.
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| Urine pH and drug elimination;;Trapped in basic environments. | Weak acids
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| Urine pH and drug elimination;;Trapped in acidic environments. | Weak bases
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| 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.
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| dose response curves and;;shifts curve to the right, decreasing potency and ↑ EC50. | competitive antagonist
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| dose response curves and;;shifts the curve downward, decreasing efficacy. | noncompetitive antago-;nist
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| 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.
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| 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.
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| 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
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| Efficacy | maximal EFFECT
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| Potency | amount needed for a given EFFECT
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| amount needed for a given EFFECT | Potency
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| maximal EFFECT | Efficacy
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| Therapeutic index | TILE;;LD50/ED50
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| pre and postsynaptic nervous system neurotransmitters;;Parasymp | ACh;(nicotinic);;ACh;(muscarinic)
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| pre and postsynaptic nervous system neurotransmitters;;Somatic | only one ;ACh (nicotinic)
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| 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
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| nicotinic receptor mech | ACh ligand gated Na+/K+ channels
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| muscarinic receptor mech | ACh G- protein coupled receptors that act through 2nd messengers
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| ACh ligand gated Na+/K+ channels | nicotinic receptor
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| ACh G- protein coupled receptors that act through 2nd messengers | muscarinic receptor
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| G-protein-linked 2nd messengers ;give G protein and major function;;α1 Receptor | q ;;↑ vascular smooth muscle contraction
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| G-protein-linked 2nd messengers ;give G protein and major function;;α2 Receptor | i ;;↓ sympathetic outflow, ↓ insulin release
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| G-protein-linked 2nd messengers ;give G protein and major function;;β1 Receptor | s ;;↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous ;humor formation
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| G-protein-linked 2nd messengers ;give G protein and major function;;β2 Receptor | s ;;Vasodilation, bronchodilation, ↑ glucagon release
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| G-protein-linked 2nd messengers ;give G protein and major function;;M1 Receptor | q ;;CNS
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| G-protein-linked 2nd messengers ;give G protein and major function;;M2 Receptor | i ;;↓ heart rate
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| G-protein-linked 2nd messengers ;give G protein and major function;;M3 Receptor | q ;;↑ exocrine gland secretions
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| G-protein-linked 2nd messengers ;give G protein and major function;;D1 Receptor | s ;;Relaxes renal vascular smooth muscle
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| G-protein-linked 2nd messengers ;give G protein and major function;;D2 Receptor | i ;;Modulates transmitter release, especially in brain
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| 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
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| G-protein-linked 2nd messengers ;give G protein and major function;;H2 Receptor | s ;;↑ gastric acid secretion
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| G-protein-linked 2nd messengers ;give G protein and major function;;V1 Receptor | q ;;↑ vascular smooth muscle contraction
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| 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
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| Given the major function and G-protein class name the receptor;;q ;↑ vascular smooth muscle contraction | α1
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| Given the major function and G-protein class name the receptor;;i ;↓ sympathetic outflow, ↓ insulin release | α2
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| Given the major function and G-protein class name the receptor;;s ;↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous ;humor formation | β1
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| Given the major function and G-protein class name the receptor;;s ;Vasodilation, bronchodilation, ↑ glucagon release | β2
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| Given the major function and G-protein class name the receptor;;q ;CNS | M1
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| Given the major function and G-protein class name the receptor;;i;↓ heart rate | M2
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| Given the major function and G-protein class name the receptor;;q ;↑ exocrine gland secretions | M3
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| Given the major function and G-protein class name the receptor;;s ;Relaxes renal vascular smooth muscle | D1
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| Given the major function and G-protein class name the receptor;;i ;Modulates transmitter release, especially in brain | D2
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| Given the major function and G-protein class name the receptor;;q ;↑ nasal and bronchial mucus production, contraction of bronchioles, | H1
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| Given the major function and G-protein class name the receptor;;s ;↑ gastric acid secretion | H2
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| Given the major function and G-protein class name the receptor;;q ;↑ vascular smooth muscle contraction | V1
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| Given the major function and G-protein class name the receptor;;s ;↑ H2O permeability and reabsorption in the collecting tubules of the kidney | V2
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| 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)."
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| 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)
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| 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])
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| 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])
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| 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.
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