Term
| Michaelis menten kinetics |
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Definition
Km is inversely related to the affinity of an enzyme for its substrate
Vmax is directly proportional to the enzyme concentration |
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Term
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Definition
1/Km is the x axis
1/Vmax is the Y axis
Inc y intercept = dec Vmax
The further to the R the x intercept, the greater the Km and the lower the affinity |
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Term
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Definition
Vd of plasma bound drugs can be altered by liver and kidney disease
Vd= amount of drug in body/plasma drug concentration
Low: 4-8L, blood, large charged molecules, plasma protein bound
Medium: ECF, small hydrophilic molecules
HIgh: All tissues, small lipophilic molecules, especially if bound to tissue protein |
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Term
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Definition
A drug infused at a constant rate takes 4-5 half lives to reach steady state
t1/2= 0.7 x Vd/CL |
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Term
|
Definition
Relates the rate of elimination to the plasma concentration
Clearance may be impaired with defects in cardiac, hepatic, or renal function
Cl= rate of elimination/plasma drug concentration
CL= 0.7xVd/(t1/2) |
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Term
|
Definition
Loading dose = Cp x Vd/F (Css x Vd)
Maintenance dose = Cp x Cl/F (Css x Cl)
In renal or liver disease, maintenance dose is decreased, but loading dose remains the same |
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Term
|
Definition
Rate of elimination is constant regardless of Cp
Cp decreases linearly with time
*Phenytoin, Ethanol, Aspirin |
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Term
|
Definition
Rate of elimination is directly proportional to the drug concentration (constant fraction of drug eliminated per unit time)
Cp decreases exponentially with time |
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Term
| Urine pH and drug elimination |
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Definition
Ionized species are trapped in urine and cleared quickly
Neutral forms are reabsorbed |
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Term
|
Definition
Phenobarbital, methotrexate, aspirin
Trapped in basic environments
Tx overdose with bicarbonate |
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Term
|
Definition
Amphetamines
Trapped in acidic environments
Tx overdose with ammonium chloride |
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Term
|
Definition
Step 1: reduction, oxidation, hydrolysis with p450 yields a slightly polar, water soluble metabolite (still active)
Geriatric patients lost step 1 first
Step 2: Glucuronidation, acetylation, sulfating usually yields very polar, inactive metabolites |
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Term
|
Definition
LD50/ED50
Safer drugs have higher TI values |
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Term
| Central and Peripheral NS |
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Definition
All first synapses are Ach mediated
*Cardiac and Sm Mm, gland cells, nerve terminals (NE, a, B), renal vasculature and smooth muscle (D1) are NOT ach mediated |
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Term
|
Definition
Nicotinic Ach receptors are ligand gated Na/K channels
Muscarinic Ach receptors are G protein coupled receptors that act through second messengers |
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Term
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Definition
Gq protein class
Inc vascular smooth muscle contraction
Inc pupillary dilator muscle contraction
Inc intestinal and bladder sphincter muscle contraction
*No heart effects |
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Term
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Definition
Gi protein class
Dec sympathetic outflow (inc vasodilation), dec insulin release, dec lipolysis, inc platelet aggregation |
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Term
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Definition
Gs protein class
Inc HR, Inc contractility, inc renin release, inc lipolysis |
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Term
|
Definition
Gs protein class
Vasodilation, bronchodilation
Inc HR, inc contractility
Inc lipolysis, inc insulin release, dec uterine tone
Ciliary muscle relazation, inc AH production |
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Term
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Definition
Gq protein
CNS, enteric nervous system |
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Term
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Definition
Gi protein
Dec HR and contractility of atria |
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Term
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Definition
Gq protein
Inc exocrine gland secretions, inc gut peristalsis
Inc bladder contractions
Bronchoconstriction, inc pupillary sphincter constriction, ciliary muscle contraction |
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Term
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Definition
D1: Gs protein
Relaxes vascular smooth muscle
D2: Gi protein
Modulates transmitter release in the brain |
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Term
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Definition
Gq protein
Inc nasal and bronchial mucus production, contraction of bronchioles, prutitis, pain |
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Term
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Definition
Gs protein
Inc gastric acid secretion |
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Term
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Definition
Gq protein
Inc vascular smooth muscle contraction |
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Term
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Definition
| Inc H2O permeability and reabsorption in the collecting tubules of the kidney |
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Term
|
Definition
HAV 1 M&M
Act PLC, convert PIP2 to DAG and IP3
DAG act PKC
IP3 inc Ca to cause sm mm contrations |
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Term
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Definition
B1, B2, D1, H2, V2
Stimulates adenylyl cyclase to convert ATP to cAMP, inc PKA, increasing Ca in the heart and blocking myosin light chain |
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Term
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Definition
MAD 2s
BLOCKS pathway: adenylyl cyclase to convert ATP to cAMP, inc PKA, increasing Ca in the heart and blocking myosin light chain |
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Term
|
Definition
Vesamicol- blocks Ach vesicle formation
Hemicholinium- blocks entry of choline into nerve terminal
Botulinum- Blocks vesicle release into synapse |
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Term
|
Definition
Metyrosine- Blocks conversion of tyrosine to DOPA
Reserpine- blocks DA vesicle formation
Guanethidine/bretylium- blocks NE vesicle release
Cocaine,TCAs, amphetamines- blocks NE reuptake
Amphetamines- stimulate NE vesicle release
a2 and M2- block vesicle release
AT2- stim vesicle release |
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Term
| Direct Cholinomimetic agonists |
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Definition
| Bethanechol, carbachol, pilocarpine, methacholine |
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Term
|
Definition
Use: Postop ileus, neurogenic ileus, urinary retention
Act: Activates bladder and bowel smooth muscle, resistant to AchE |
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Term
|
Definition
Use: glaucoma, pupillary contraction and relief of IOP
Act: carbon copy of Ach |
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Term
|
Definition
Use: Potent stimulator or sweat, tears and saliva; open and closed angle glaucoma
Act: Contracts ciliary muscles, pupillary sphincter, resistent to AchE |
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Term
|
Definition
Use: challenge test for asthma
Act: Stimulates muscarinic receptors in airway when inhaled |
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Term
| Indirect cholinomimetic agonists |
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Definition
| Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Donepezil |
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Term
|
Definition
Use: Post op and neurogenic ileus, urinary retention, MG, reversal of NMJ blockade
Act: Inc endogenous Ach
Neo CNS = NO CNS penetration |
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Term
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Definition
Use: MG (long acting), does not penetrate CNS either
Act: Inc endogenous Ach, inc strength |
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Term
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Definition
Use: Diagnose MG (short acting)
Act: Inc endogenous Ach |
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Term
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Definition
Use: Anticholingeric toxicity, crosses the BBB
Act: inc endogenous Ach, fixes atropine overdose |
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Term
|
Definition
Use: Alzheimers disease
Act: inc endogenous Ach |
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Term
| Cholinesterase inhibitor poisoning |
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Definition
DUMBBELSS
Often due to Organophoshate poisoning
Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation, lacrimation, sweating, salivation (WET)
Tx: atropine and pralidoxime |
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Term
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Definition
| Atropine, homatropine, tropicamide, benztropine, scopolamine, ipatropium, tiotropium, oxybutynin, glycopyrrolate |
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Term
| Atropine, homatropine, tropicamide |
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Definition
Eye
Produce mydriasis and cycloplegia |
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Term
|
Definition
CNS
For parkinsons disease |
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Term
|
Definition
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Term
|
Definition
Respiratory
COPD and asthma |
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Term
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Definition
GU
Reduce urgency in mild cystitis and reduce bladder spasms |
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Term
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Definition
GI, respiratory
Preoperative use to decrease airway secretions
Oral: drooling, peptic ulcer |
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Term
|
Definition
Muscarinic antagonist used to tx bradycardia and for opthalmic applications
Inc pupil dilation, dec airway secretions, dec acid secretion, dec motility, dec urgency in cystitis
*blocks DUMBBELSS, EXCEPT for CNS and Sk Mm excitation because they are nicotinic mediated |
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Term
|
Definition
Inc body temp, rapid pulse, dry mouth, dry flushed skin, cycloplegia, constipation, disorientation
Hot as a hare, dry as a bone, red as a beet, blind as a bat and mad as a hatter
Jimson weed can cause this same symptoms in Gardeners |
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Term
|
Definition
a1, a2, B1, B2 activity
Low dose: more alpha activity
High dose: more beta activity, leads to inc BP and HR
Anaphylaxis, glaucoma (open angle only), asthma and hypotension |
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Term
|
Definition
Mostly a1, a2.. some B1
Used in hypotension (but decreases renal perfusion) |
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Term
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Definition
B1, B2
Torsades de pointes, bradyarrythmias |
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Term
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Definition
Low dose: D1 only
Med dose: B1, B2
High dose: a1, a2
Shock (renal perfusion), heart failure, inotropic and chronotropic |
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Term
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Definition
Mostly B1
Heart failure, cardiac stress testing, inotropic and chronotropic |
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Term
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Definition
a1, a2
Hypotension (causes vasoconstriction), ocular procedures, rhinitis |
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Term
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Definition
mostly B2, but some B1
Terbutaline is for reducing premature uterine contractions |
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Term
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Definition
Only B2
Reduces premature uterine contractions |
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Term
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Definition
| Indirect general agonist, releases stored catecholamines |
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Term
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Definition
Indirect general agonist, releases stored catechoalmines
Nasal decongestion, urinary incontinence, hypotension |
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Term
|
Definition
Indirect general agonist, reuptake inhibitor
Causes vasoconstriction and local anesthesia
*never give B blocker, can lead to unopposed a1 hypertension |
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Term
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Definition
NE causes an increase in systolic and diastolic pressures via a1 vasoconstriction > inc mean arterial pressure > bradycardia
Isoproterenol causes B2 mediated vasodilation, resulting in MAP decrease and inc HR through B1 and reflex activity |
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Term
|
Definition
Clonidine, a-methyldopa
Centrally acting a2 antagonists, decreasing central sympathetic outflow
HTN with renal disease (no decrease in BF to kidney) |
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Term
|
Definition
| Phenoxybenzamine, phentolamine, prazosin, mirtazepine |
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Term
|
Definition
Irreversible non selective alpha blocker
Pheochromocytoma > use to blocks a release HTN
Tox- orthostatic HTN, reflex tachy |
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Term
|
Definition
Reversible Non selective alpha blocker
Give to patients on MAO inhibitors who eat tyramine containing foods |
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Term
| Prazosin, terazosin, doxazosin, tamsulosin |
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Definition
Alpha 1 selective blocker
HTN, urinary retention in BPH
Tox- orthostatic hypotension, dizziness, HA |
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Term
|
Definition
Alpha 2 selective blockers
Depression
Tox- increases appetite, inc serum cholesterol
Good for elderly and anorexic patients |
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Term
|
Definition
Angina pectoris- dec HR and CT > dec O2 demand
MI- Dec mortality (carvediolol and metropolol)
SVT- Dec AV conduction velocity (metropolol, esmolol)
HTN- Dec CO, dec renin (B1 block on JGA cells)
CHF- Slows progression of HF
Glaucoma- dec secretion of AH (timolol) |
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Term
| B blocker toxicity and selectivity |
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Definition
Tox- impotence exacerbation of asthma (block B2 bronchodilation), seizures, sedation, sleep alterations, mask hypoglycemia
A > M: B1 selective, good for COPD pts
N > Z: NS
Carvedilol, labetalol: NS with alpha blocking effects
Partial B agonists: Pindolol, acebutolol |
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Term
|
Definition
Salicylates- NaHCO3
Amphetamines- NH4Cl
Antimuscarinic/anticholinergic- physostigmine
B blockers- glucagon
Cyanide- nitrites, thiosulfate, hyroxycobalamin
Methanol, ethylene glycol- fompizole
Benzos - Flumazenil
TCAs- NaHCO3
tPA- aminocaproic acid
Theophylline - B blocker |
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Term
|
Definition
| cocaine, sumatriptan, ergot alkaloids |
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Term
|
Definition
| Vancomycin, adenosine, niacin, Ca Ch blockers |
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Term
|
Definition
| Doxorubacin, daunorubicin |
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Term
|
Definition
| Sotalol, quinidine antiarrythmics |
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Term
|
Definition
| Clonidine, carbamazepine, colchicine, PTU, methimazole, dapsone |
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Term
|
Definition
| Chloramphenicol, benzene, NSAIDs, PTU, methimazole |
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Term
| Direct Coombs pos hemolytic anemia |
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Definition
|
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Term
|
Definition
|
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Term
| Hemolysis in G6PD patients |
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Definition
| Sulfa drugs, Isoniazid, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin |
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Term
|
Definition
| Phenytoin, Methotrexate, Sulfa drugs |
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Term
|
Definition
| Bleomycin, Amiodarone, Busulfan |
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Term
| Acute cholestatic hepatitis, jaundice |
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Definition
|
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Term
| Focal to massive hepatic necrosis |
|
Definition
| Halothane, Amantia phylloides, VPA, acetaminophen |
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Term
|
Definition
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Term
|
Definition
|
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Term
|
Definition
| Spironolactone, Digitalis, Ketoconazole, Cimetidine, alcohol, estrogens |
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Term
|
Definition
|
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Term
|
Definition
| Niacin, tacrolimus, PIs, HCTZ, corticosteroids |
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Term
|
Definition
| Lithium, amiodarine, sulfonamides |
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Term
|
Definition
| Glucocorticoids, Protease inhibitors |
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Term
|
Definition
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Term
|
Definition
| Furosemide, thiazides, niacin, cyclosporine |
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Term
|
Definition
| Fibrates, Niacin, Colchicine, Hydroxychlorquine, inteferon-a, peniclliamine, statins, glucocorticoids |
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Term
|
Definition
| Sulfonamides, Amiodarine, Tetracylcines |
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Term
|
Definition
| Pencillin, ethosuxamide, carbemazapine, Sulfa drugs, lamotrigine, allopurinol, Phenytoin, phenobarbitol |
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Term
|
Definition
| Hydralazine, INH, Procainamide, Phenytoin (HIPP) |
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
| Cyclophosphamide, isosfamide (prevent with mesna) |
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Term
|
Definition
| Methicillin, NSAIDs, furosemide |
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Term
|
Definition
| Carbamazepine, cyclophosphamide |
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Term
|
Definition
|
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Term
|
Definition
| Antipsychotics, reserpine, metoclopramide |
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Term
|
Definition
| Isoniazid, buproprion, imipenem/cilstatin, tramadol, enflurane, metoclopramide |
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Term
|
Definition
| Atropine, TCAs, H1 blockers, neuroleptics |
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Term
|
Definition
| Metronidazole, certain cephalosporins, procarbazine, 1st gen SUs |
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Term
|
Definition
| Aminoglycosides, vancomycin, loop diuretics, cisplastin |
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Term
|
Definition
Modafenil, Barbituates, St Johns Wort, Phenytoin, Rifampin, Griseofulvin, Carbmazapine, Chronic alcohol use
"Momma Barb steals Phen-phen and refuses greasy carbs chronically for induction into the club" |
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Term
|
Definition
| Macrolides, amiodarone, Grapefruit juice, Isoniazid, Cimetidine, Ritonavir, Acute alcohol abuse, Ciprofloxacin, Ketoconazole, Sulfonamides, Gemfibrozil, Quinidine |
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Term
|
Definition
| Probenacid, Furosemide, Acetazolamide, celecoxib, thiazides, sulfonamides antibiotics, sulfasalazine, SUs |
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