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[h] General Pharmacology Flashcards
[i] Master this session in just 5 minutes.
[q] ……… is the time to eliminate 50% of a given amount (or to decrease plasma level to 50% of a former level).
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IHQxLzIu[Qq]
[q] Which type of elimination rate?
– A constant amount of drug is eliminated per unit time.
– t1/2 is a variable.
– Drugs include ethanol (except low blood levels), phenytoin (high therapeutic doses), and salicylates (toxic doses).
– High risk of drug accumulation.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFplcm8tT3JkZXIgRWxpbWluYXRpb24gUmF0ZS4=
Cg==Cg==[Qq][q] Which type of elimination rate?
– A constant fraction of the drug is eliminated per unit time.
– Rate of elimination is directly proportional to plasma level (or the amount present). The higher the amount, the more rapid the elimination.
– t1/2 is a constant.
– Low risk of drug accumulation.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IEZpcnN0LU9yZGVyIEVsaW1pbmF0aW9uIFJhdGUu
Cg==Cg==[Qq][q] ……… is reached when rate in = rate out of the drug, usually reached clinically after 4–5 t1/2.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFN0ZWFkeSBzdGF0ZS4=
Cg==Cg==[Qq][q] …….. is one time dose and is estimated to put into the body the amount of drug that should be there at a steady state.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IExvYWRpbmcgZG9zZS4=
Cg==Cg==[Qq][q] …….. = .7 X Vd/Cl
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IHQxLzIu
Cg==Cg==[Qq][q] …… = Cl XCss X Dosing interval / f
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IE1haW50ZW5hbmNlIGRvc2Uu
Cg==Cg==[Qq][q] …….. = Vd X Cp / f
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IExvYWRpbmcgZG9zZS4=
Cg==Cg==[Qq][q] Km is a measure of the affinity of the enzyme for its substrate. When comparing two enzymes, the one with the higher Km has a ………. affinity for its substrate.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IGxvd2VyLg==
Cg==Cg==[Qq][q] ………. is the maximum rate possible to achieve with a given amount of enzyme. The only way to increase it is by increasing the [E].
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFZtYXgu
Cg==Cg==[Qq][q] If the x-intercept shifts to the right → ↑ Km → ↓ For example: – : -2 → 1, this means Km will (increase or decrease) and affinity will (increase or decrease).
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IGluY3JlYXNlLCBkZWNyZWFzZS4=
Cg==Cg==[Qq][q] If the y-intercept shifts to the downward → ↑ Vmax → ↑ reaction rate. For example: : 2 → 1, this means Vmax will (increase or decrease).
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IGluY3JlYXNlLg==
Cg==Cg==[Qq][q] …….. is the ability of drug to bind to receptor, shown by the proximity of the curve to the y axis (if the curves are parallel).
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IEFmZmluaXR5LiBUaGUgbmVhcmVyIHRoZSB5IGF4aXMsIHRoZSBncmVhdGVyIHRoZSBhZmZpbml0eS4=
Cg==Cg==[Qq][q]……. shows relative doses of two or more agonists to produce the same magnitude of effect, again shown by the proximity of the respective curves to the y axis (if the curves do not cross).
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFBvdGVuY3ku
Cg==Cg==[Qq][q]……….. is a measure of how well a drug produces a response (effectiveness), shown by the maximal height reached by the curve.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IEVmZmljYWN5Lg==
Cg==Cg==[Qq][q] ………. decrease the affinity and potency without change on efficacy. Can be overcomed by increasing the substrate concentration.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IENvbXBldGl0aXZlIGFudGFnb25pc3Qu
Cg==Cg==[Qq][q] ……… decrease the efficacy without change on affinity and potency of the reaction. Cann’t be overcomed by increasing the substrate concentration.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IE5vbmNvbXBldGl0aXZlIGFudGFnb25pc3Qu
Cg==Cg==[Qq][q] ……… act as agonist without full efficacy when used alone, and as antagonist in presence of full agonist.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFBhcnRpYWwgYWdvbmlzdC4=
Cg==Cg==[Qq][q] ……… = ED50/TD50 and permit evaluation of the relative safety of a drug.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFRoZXJhcGV1dGljIEluZGV4Lg==
Cg==Cg==[Qq][q] Rebound rhinorrhea is associated with the use of topical decongestants for > 3 days. The use of adrenergic agonists should be stopped to allow the restoration of normal norepinephrine feedback pathways.
[c]IFNob3cgbWUgdG hlIGFuc3dlcg==[Qq]
[f]IFJlYm91bmQgcmhpbm9ycmhlYS4=[Qq]
[x][restart]
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