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2- General Pharmacology 2 (2 Hours & 30 minutes)

Topic Progress:

[vdo id=’a42b35c92c4a4c888a2b1e18f156b800′]

 

   Content of this Session
    • Elimination
    • Michaelis-Menten Equation
    • Lineweaver-Burk Equation
    • Full and Partial Agonists
    • Duality of Partial Agonists:
    • Antagonism and Potentiation:
    • Pharmacologic antagonism
    • Toxicity and the Therapeutic Index (TI)
    • Types of drug interactions

 

 

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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).

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[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.

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[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.

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[q] ……… is reached when rate in = rate out of  the drug, usually reached clinically after 4–5 t1/2.

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[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.

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[q] …….. = .7 X Vd/Cl

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[q] …… = Cl XCss X Dosing interval / f

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[q] …….. = Vd X Cp / f

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[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.

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[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].

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[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).

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[q] If the y-intercept shifts to the downward → ↑ Vmax → ↑ reaction rate. For example: : 2 → 1, this means Vmax will (increase or decrease).

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[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).

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[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).

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[q]……….. is a measure of how well a drug produces a response (effectiveness), shown by the maximal height reached by the curve.

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[q] ………. decrease the affinity and potency without change on efficacy. Can be overcomed by increasing the substrate concentration.

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[q] ……… decrease the efficacy without change on affinity and potency of the reaction. Cann’t be overcomed by increasing the substrate concentration.

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[q] ……… act as agonist without full efficacy when used alone, and as antagonist in presence of full agonist.

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[q] ……… = ED50/TD50 and permit evaluation of the relative safety of a drug.

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[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.

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[x][restart]

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