Pharm Flashcards
Km is
inversely related to the affinity
Vmax is
Directly proportional to enzyme concentration
Increase y-intercept on Lineweaver-Burk plot means
Decrease in Vmax
Competitive inhibiotrs do what on a Lineweaver-Burk plot
Bring Km closer to 0
No change to Vmax (y-intercept)
Bioavailability (F)=
AUCo / AUCIV
Volume of distribution (Vd) =
Dose / [P]
Drug with low Vd found in
Blood
Drug with medium Vd found in
ECF
Drug with High Vd found in
All tissues
t1/2=
[0.7 X Vd] / Cl
Cl=
Rate of elimination / [P]
Vd X K
Loading dose=
[Cp x Vd] / F
Maintenance dose=
[Cp x Cl x τ] / F
Zero PEAs for me
Drugs with zero order of elimination
- Phenytoin
- Ethanol
- Asprin
Phase 1 drug metabolism
- Reduction
- Oxidation
- Hydrolysis with P-450
Phase 2 drug metabolism
- Glucuronidation
- Acetylation
- Sulfation
Efficacy is
Maximal effect a drug can produce
Potency is
Amount of drug needed for a given effect
α1 major functions
- Gq
- Increase vascular smooth muscle contraction
- Increase pupillary dilator muslce contraction (Mydriasis)
- Increase intestinal and bladder sphincter muscle contraction
α2 major function
- Gi
- Decrease symathetic outflow
- Decrease insulin release
- Decrease lipolysis
- Increase Platelet aggregation
Hemicholinium action
Inhibits Choline uptake
Vesamicol action
Inhibits ACh storage
Botulinum action
Inhibit ACh release
Metyrosine action
Inhibit formation of DOPA from Tyrosine
Reserpine action
Inhibit storage of NE
Bretylium action
Inhibits release of NE
Amphetamine action
Increase release of NE
Cocaine and TCA action
Inhibit reuptake of NE
Cholinomimetic direct agonists
- Bethanechol
- Carbachol
- Pilocarpine
- Methacholine
Bethanechol clinical use
- Post-op ileus
- Neurologenic ileu
- Urinary retention
Pilocarpine used for
Open-angle and closed-angle glaucoma
Methacholine used for
Challenge test for diagnosis of asthma
Anticholinesterases (7)
- Neostigmine
- Pyridostigmine
- Physostigmine
- Donepezil
- Rivastigmine
- Galantamine
- Edrophonium