Pharmacology Flashcards
Km
proportional to 1/affininty of enzyme of substrate
Vmax
proportional to enzyme conc
Vd=
amount of drug in body/plasma conc
Clearance
rate of elimination of drug/plamsa drug conc: Vd*Ke (elimination constant)
Half life
t1/2=0.7*Vd/Clearance
Loading dose/maintenance dose
Loading dose=CpVd/F, Maintenance dose=CpCL*dosage interval/F
Amount of half lives to reach steady state
4-5 half lives
What is dosage interval constant and Cp constant
Dosage interval (time between doses), if not administered continuously Cp-target plasma concentration in steady state
3 drugs that have zero order elimination
Phenytoin, Ethanol, Aspirin
Treat weak acid overdose with?
Bicarbonate
Treat weak base overdose with?
Ammonium chloride
Phase geriatric patients lose first?
Phase I
Therapeutic index equation
TD50/TE50=median toxic tose/median effective dose
Drugs with lower therapeutic index
Digoxin, warfarin, lithium, theophylline “THEO, DIEGO went to WAR over LITHIUM”
Competitive antagonist example
Diazepam (agonist + flumazenil (competitive antagonist) on GABA receptor
Noncompetitive antagonist example
Norepinephrine (agonist) + phenoxybenzamine (noncompetitive antagonist on alpha receptor)
Example of partial agonist
Morphine (full agonist) vs. buprenorphine (partial agonist) at opioid mu receptors
Prevents ACh packaging in vesicles
Vesamicol
Prevents NE release for noradrenergic axon
a2 negative feedack, bretylium, guanethidine
Prevents tyrosine to DOPA conversion
metyrosine
Postoperative ileus, neurogenic ileus, urinary retention
Bethanechol
Constricts pupil and relieves intraocular pressure in glaucoma
Carbachol
Challenge test for diagnosis of asthma
Methacholine
Potent stimulator of sweat, tears, and saliva. Open- and closed angle glaucoma. Open angle constricts what and close angle constricts what?
Pilocarbine
Open-ciliary muscle contraction
Closed-pupillary sphincter muscle contraction
Alzheimer disease help increasing ACh
Donepezil, galantamine, rivastigmine
Diagnosis of myasthenia gravis
Edrophonium (extremely short acting
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade (post operative)
Neostigmine
AChe that penetrates CNS
Physostigmine
AChe that does not penetrate CNS
Neostigmine
When giving cholinomimetic agents, what 3 things do you have to watch out for exacerbation of
COPD, asthma, peptic ulcers
Organophosphate poisoning symptoms and what does it inhibit
Irreversible inhibits AChe
Diarrhea, Urination, Miosis, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation
Atropine vs Pralidoxime
Atroprine reverses muscaraninc effects but does not prevent development of nicotinic effects such as muscle paralysis
Pralidoxime is only medication that reverses both muscarininc and nicotinic effects of organophosphates
Produces mydriasis and cycloplegia
Atropine, homatropine, tropicamide
Treats acute dystonia in parkinson
Benztropine
Use parenterally: preoperative use to reduce airway secretions. Orally: drooling, peptic ulcer
Glycopyrrolate
Antispasmodic for irritable bowel syndrome
Hyoscyamine, dicyclomine
Used for COPD, asthma to help decrease bronchoconstriction
Ipratropium, tiotropium
Reduces bladder spasms and urge urinary incontinence (overactive bladder)
Oxybutynin, solifenacin, tolterodine
Used for motion sickness
Scopolamine
Atropine poisoning treatment
Physostigmine
Used to treat bradycardia and for ophthalmic applications
Atropine
Atropine effects on
Eye, airway, stomach, gut, bladder
Mydriasis+cycloplegia, decrease secretions, decrease acid production, decrease motility, decrease urgency in cystitis
Atropine toxicity
increase temp, dry, flushing, cycloplegia, disorientation
Consequence of mydriasis in atropine toxicity
angle-closure glaucoma
Hot feels cold and cold feels hot diagnosis
temperature related dysesthesia specific finding for ciguatoxin from ciguatera fish poisoning
Toxin that binds fast voltage-gated Na+ channels in cardiac and nerve tissue, preventing depolarization
Tetrodotoxin
MOA of patient with anaphylaxis like presentation who consumed dark meet fish and reasoning
Histidine in enteric system converted via bacterial histidine decarboxylase to histamine and histamine is not degraded by fish.
Used for acute asthma
Albuterol
Used for long term asthma and COPD control
Salmeterol
Albuterol, salmeterol receptor effect
B2>B1
Dobutamine
B1>B2, alpha
Dopamine
D1=D2>B>alpha
Epinephrine
B>alpha
Isoproterenol
B1=B2
Norepinephrine
alpha1>alpha2>beta1
Phenylephrine
alpha1>alpha2
Hypertensive urgency, ADHDm tourette syndrome
Clonidine
Hypertenision in pregnancy
alpha methyl dopa
Used to treat pheochromocytoma (preoperatively) to prevent catecholamine (hypertensive) crisis and MOA
Phenoxybenzamine via alpha blockade
Used to treat patients who eat tyramine-containing foods who are on MAO inhibitors
Phentolamine
Used for depression and is a alpha 2 selective antagonist
Side effects?
Mirtazapine
Sedation, increase serum cholesterol, increase appetite
Urinary symptoms of BPH
Side effects?
Terazosin, tamsulosin
1st dose orthostatic hypotension, dizziness, headache
Toxin:Acetaminophen
Antidote/treatment:
N-acetylcystenine (replenishes glutathione)
Toxin: AChE inhibitor/organophosphate
Antidote/treatment:
Atropine>pralidoxime
Toxin: Amphetamines
Antidote/ treatment:
NH4Cl
Toxin: Antimuscarinic, anticholinergic agents
Antidote/treatment:
Physostigmine
Toxin: Benzodiazepines
Antidote/treatment:
Flumazenil
Toxin: Beta blockers
Antidote/treatment:
Glucagon
Toxin Carbon monoxide
Antidote/treatment:
Hyperbaric oxygen
Toxin: Copper, arsenic, gold
Antidote/treatment:
Penicillamine
Toxin: Cyanine
Antidote/treatment:
Nitrite+thiosulfate, hydroxocobalamin
Digitalis (digoxin)
Antidote/treatmetn
Anti-dig Fab fragments
Heparin
Antidote/treatment
Protamine sulfate
Iron
Antidote/treatment
Deferoxamine, deferasirox
Lead
Antidote/treatment
EDTA, dimercaprol, succimer.
Toxin: Mercury, arsenic gold
Antidote/treatment
Dimercaprol
Methanol, ethylne glycol
Antidote/treatment
Fomepizol>ethanol
Methemoglobin
Antidote/treatment
Methylene blue, vitamin C
Opioids
Antidote/treatment
Naloxone, naltrexone
Salicylates, TCA
Antidote/treatment
NaHCO3
tPA, streptokinase urokinase
Antidote/treatment
Aminocaproic acid
Warfarin
Antidote/treatment
Vitamin K (delayed) fresh frozen plasma (immediate)
Category: azole
Ergosterol synthesis inhibitor
Category: bendazole
Antiparasitic/antihelmintic
Category: cillin
Peptidoglycan synthesis inhibitor
Category: cycline
Protein synthesis inhibitor
Category ivir
Neuraminidase inhibitor
Category: navir
Protease inhibitor
Category: ovir
DNA polymerase inhibitor
Category: thromycin
Macrolide antibiotic
Category: ane
Inhalaed anesthetic
Category: azine
Typical antipsychotic
Category: barbital
Barbiturate
Category: caine
Local anesthetic
Category: etine
SSRI
Category: ipramine, triptyline
TCA
Category: triptan
5HT 1B/1D agonists
Category: zepam, zolam
Benzodiazepine
Category: chol
Cholinergic agonist
Category: curium, curonium
Nondepolarizing paralytic
Category: olol
Beta blocker
Category: stigmine
AChe inhibitor
Category: terol
B2 agonist
Category: zosin
alpha1 antagonist
Category: afil
PDE5 inhibitor
Category: dipine
Dihydropyridine calcium channel blocker
Category: pril
ACE inhibitor
Category: sartan
Angiotensin-II receptor blocker
Category: statin
HMG-CoA reductase inhibitor
Category: dronate
Bisphosphonate
Category: glitazone
PPAR-gamma activator
Category: prazole
proton pump inhibitor
Category: prost
Prostaglanding analog
Category: tidine
H2 antagonist
Category: tropin
Pituitary hormone
Category: ximab
Chimeric monoclonal Ab
Category: zumab
Humanized monoclonal Ab
CP450 Inducers
Griseofulvin, Carbamazepine, Phenytoin, Barbiturates, Rifampin, St. Johns wort, Chronic alcoholism “Guinness, Corona, and PBRS induce chronic alcoholism”
CP450 inhibitors
Cimetidine, Ritonavir, AMiodarone, Ciprofloxacin, Ketoconazole, Acute alcohol use, Macrolides, Isoniazid, Grapefruit juice, Omeprazole, Sulfonamides “CRACK AMIGOS”
Substrates for CYP450
Anti-epileptics, Theophylline, Warfarin, OCPs (Always Think When Outdoors)
Sulfa drugs
Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotitics, Sulfasalazine, Sulfonyurease (Popular FACTSSS)
Release of ACh at NMJ depends on what ion to allow for release?
Ca2+ influx into presynaptic terminal secondary to VG calcium channels opening when action potential depolarizes causing influx of extracellular calcium
How can there be peripheral blood vessel vasodilation even though blood vessels do not have cholinergic innervation?
Muscarinic agonists are present on endothelial surface binding cholinomimetic agents to these receptors that promotes release of NO (EDRF). NO activates guanylate cyclase–>increase intracellular cGMP. cGMP acticates Ca pump and causes Ca efflux from cell and with decrease calcium concentration–>vascular smooth muscle relaxation
What channel does cocaine block preventing its reuptake?
Na+/K+ ATPase
Why do non-selctive blockers exacerbate hypoglycemia?
They mask its adrenergic symptoms and for this reason should not be used in diabetes mellitus. Adrenergic symptoms include sweating tremor palpitations hunger nervounsess due to NE/ Epi release. Non-selective B-blockers inhibit compensatory reactions to hypoglycemia by blocking NE/Epi. Instead, selective B1 antagonists should be used because they dont block metabolic sympathetic effects
B-blocker used for CHF
Nonselective (carvedilol, labetolol)