Pharmacology General Flashcards
Drugs with zero order elimination?
PEA– Phenytoin; Ethanol; Aspirin
Treat base overdoses with?
Amonium chloride
Phase 1 drug metabolism?
Reduction, oxidation, hydrolysis with cyp P450– usually yields slightly polar water soluble metabolites
Phase 2 metabolism?
Conjugation– glucuronidation; acetylation; sulfation
Efficacy vs potency?
Efficacy– maximal effect a drug can produce
Potency– amount of drug needed to produce an effect
Competitive antagonists shift curve?
To the right– decrease the potency (Diazepam+flumazenil on GABA)
Noncompetitive antagonist shifts curve?
Down– decreases efficacy
NE+phenoxybenzamine on alpha receptors
Partial agonist?
Reduce efficacy– potency can go up or down
therapeutic index?
Median lethal dose over median effective dose
Lineweaver burk plot– what happens if my point moves more to the right? i.e. greater x intercept?
The greater the Km and the lower the affinity
What happens if my x intercept gets smaller in the lineweaver burk plot?
Lower Km and higher affinity
Volume of distribution
Amount of drug in body/plasma drug concentration
Half life?
(.7*Vd)/Clearance
Adrenal medulla and sweat glands are innervated by?
Cholinergic fibers even though they are SYMPATHETIC
Muscarinic receptors are of what type?
GPCR (M1-M5)
Parasympathetics act on?
Cardiac and smooth muscle, glands, and nerve terminals
Mechanism of Gq?
Phospholipase c converts lipids into PIP2 which can go to
1) IP3–>inc Ca–>smooth muscle contraction
2) DAG–>protein kinase C
Mechanism of Gs/Gi?
Adenylyl cyclase converts ATP to cAMP–>protein kinase A which 1) blocks myosin light chain kinase and 2) increases Ca in heart
Qiss Qiq (till you’re) siq (of) Sqs?
alpha 1,2 beta1,2 M1,2,3 D1,D2 H1, H2 V1, v2
Increases vascular smooth muscle contraction?
alpha 1
increases pupillary dilator muscle?
alpha 1
Increases gastic acid secretion?
H2
Relaxes renal vascular smooth muscle?
D1
Dec insulin release? and dec lipolysis
alpha2
Increase insulin release? and inc lipolysis
beta2
Bronchodilation and tocolytic?
Beta 2
Ciliary muscle relaxation?
Beta 2
Increase platelet aggregation?
alpha 2
dec hr and contractility of atria?
M2
Increases lacrimal productoin (exocrine gland)?
M3
Increase bladder contraction?
M3
Bronchoconstriction?
M3
miosis and ciliary muscle contraction (i.e. accommodation)
M3
Pruritus?
H1
Intestinal and bladder sphincter muscle contraction?
alpha1
Epi effects blank more than blank?
Beta more than alpha
Norepi effects blank more than blank?
alpha more than beta
Increase aqueous humor production?
beta2
M3 rhyme?
M3 makes you pee (parasymp)
Blocks tyrosine to dopa?
Metyrosine
Blocks packaging of dopamine?
reserpine
Blocks reuptake of NE?
Cocaine, TCA, and amphetamine
Guanethidine and bretylium?
block NE release from presynaptic
NE acts on blank to autoregulate itself?
Alpha 2
Blocks choline uptake?
Hemicholinium
Blocks ACh from moving into vesicles?
Vesamicol
Urinary retention and postoperative ileus?
Bethanechol– Beth, call me if you want to pee or crap
Carbachol?
Glaucoma, pupillary contraction; CARBon copy of AcetylCHOLINE
Stimulator of sweat, tears, and saliva, and open and closed glaucoma?
PILOcarpine– RESISTANT TO AChE
you cry, drool, and sweat on your PILlow
Long acting drug for myasthenia gravis?
Pyridostigmine– pyRIDostiGM– gets rid of MG
Indirect anticholinesterase that crosses blood brain barrier?
Physostigmine– PHYSO PHYXES atropine overdose
AChEI for Alzheimers?
Donepezil
What should you be careful about exacerbating with cholinomimetic agents?
COPD, Asthma, and Peptic ulcers
Side effects of cholinesterase inhibitor drugs?
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating and Salivation
Antidote to cholinesterase inhibitor toxicity?
Atropine+ pralidoxime
Benztropine
Muscarinic antagonist for parkinsons
Scopolamine?
Motion sickness– need SCOPolamine if we’re going to drive around SCOPing out the scene in New brunswick
Ipratropium, tiotropium?
I PRAy I can breath soon– asthma and copd
Oxybutynin?
Reduces bladder spasms– oxybladdertynin
Glycopyrrolate?
Preoperative use to reduce airway secretions or drooling, peptic ulcer— glycoPYRROLate for Peptic ulcer
Deleterious effect of atropine in elderly?
Can cause acute angle closure glaucoma
Epinephrine?
Alpha, and beta– NO D1– used for anaphylaxis, glaucoma, asthma, and hypotension
increases HR and BP
Norepi?
Alpha>beta (no beta 2 or D1)– used for hypotension (decreases renal perfusion)— causes increase in diastolic and systolic pressures
Isoproterenol?
All Beta– Torsades, bradyarrhythmias (but can worse ischemia)— IsoPROterenol is PRO BRO i.e. pro Beta
Decreases BP via B2 and Inc HR via B1 and reflex activity
Dopamine uses?
Shock, heart failure, inotropic and chronotropic
Cardiac stress testing?
Dobutamine (mostly b1)– doBETAmONE– also used for heart failure
Mydriatic effect, only act on alpha 1 and 2?
Phenylephrine– used as decongestant as well
Albuterol/Terbutaline
Beta agonists (Terbetaline)
Acts on B2 only and reduces premature uterine contractions?
Ritodrine prevents UteRINE (ritodrine rhymes with uterine)
Used to treat narcolepsy?
Amphetamines
Sympathoplegic used in hypertension in a person with renal disease?
Clonidine– centrally acting alpha 2 agonists
clonidine decreases central sympathetic outflow
Phenoxybenzamine?
Phenoxy for Pheo– alpha blocker– may cause orthostatic hypotension or reflex tachycardia
Phentolamine?
alpha blocker– give to patients on MAO inhibitor
Too much PHEN (fun) at the wine and cheese party, will take it’s TOL and you’ll need PHENTOLAMINE
Patient comes to you with insomnia. You give her an alpha 2 selective blocker– what is the drug? what are the side effects?
Drug is Mirtazapine and side effects are inc serum cholesterol and inc appetite
Difference between Epinephrine and Phenylephrine?
Epi has alpha AND beta response
Phenylephrine only has Alpha
These beta blockers should be used in those with pulmonary disease?
A BEAM
Acebutolol, btaxolol, esmolol, atenolol, metoprolol
Carvedilol?
nonselective alpha and beta antagonist
Clearance?
Rate of elimination/plasma drug concentration
Loading dose?
Vd*CSS
Maintenance Dose?
css*cl
amphetamine overdose
NH4Cl
Beta blocker overdose
glucagon
Digitalis overdose
Lidocaine, mg2+, normalize K+
Arsenic and gold overdose
Dimercaprol; succimer and penicillamine
copper
penicillamine
theophylline overdose
Beta blockers
drug that can cause acute cholestatic hepatitis
erythromycin (maCro)
gingival hyperplasia
phenytoin and verapamil and cyclosporin
photosensitivity
sulfonamides amiodoroaone tetracycline
drug that can cause fanconi syndrome
tetracycline
Can cause torsades
Some risky meds can prolong qT
Sotalol; Risperidone; Mcrolides; chloroquine; protease inhibitors; quinidine thiazides