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265 Cards in this Set

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How do Vmax differe between competitive and noncompetitive inhibitors
competitive - unchanged
noncompetitive - decreased
How do Km differ between competitive and noncompetitive inhibitors
compeittive - increase
noncompetitive - unchanged
how are pharmacodynamics affected by competitive inhibitors
decrease in potency
how are pharmacodynamics affected by noncompetitive inhibitors
decrease in efficacy
what is the formula for volume of distribution
amount of drug in the body/plasma drug concentration
where is a low volume of distribution held
in blood
where is a medium volume of distribution held
extracellular space or body water
where is a high volume of distribution held
distributed to all tissues
what are the two formula's for clearence
- rate of elimination of drug/plasma drug conc

- Vd x Ke (elimination constant)
how many half-lifes does it take to reach steady state
4-5
wha tis the formula for half life
t1/2 = (0.7 x Vd)/ CL
what is the formula for loading dose
Cp X (Vd/F)
what is the formula for maintenance dose
Cp x (CL/F)
how are maintence and loading dose affected in renal and liver disease
maintence dose decreases and loading dose is unchanged
what are three examples of zero order drugs
- Phenytoin
- Ethanol
- Asprin (at high or toxic conc)
what is rate of elimation equal to in first order reaction
- drug concentration
how does target plasma concentration change during first order reactions
- decreases exponentially
What three things occur during phase 1 metabolism and what metabolites are made
- oxidation, reduction, hydrolysis
- yields slightly polar and water soluble metabolites
What three things occur during phase 2 metabolism and what metabolites are made
- acetylation, glucuronidation, sulfation
- Yields very polar, inactive metabolites which are normal excreted
what is efficacy
maximal effect a drug can produce
what is potency
amount of drug needed for a given effect
what is the effect of a competitive antagonisist
- shifts curve to right and decreases potency with no change in efficacy
what is the effect of a noncompetitive antagonist
- shifts curve down and decreases efficacy
what is the effect of a partial agonist
- acts at same site as full agonist but with reduced maximal effect and decreased efficacy
- potency can increase or decrease
what is physiologic antagonism
substance that produces the opposite physiologic effect of an agonist but does not act at the same receptor
what is the formula for therapeudic index
LD50/ED50
what are the adrenal medulla and sweat glands innervated by
cholinergic fibers and the sympathetic NS
what type of receptors are nicotinic ACh
ligand-gated Na+/K+ channels
what type of receptors are muscarinic ACh receptors
G-protein-coupled receptors
what are the three major functions of alpha 1 receptors
- icnreased vascular smooth muscle contraction
- increased pupillary dilator muscle contraction
- increased intestinal and bladder sphincter muscle contraction
what is mydriasis
dilation of pupil
what are the two main functions of alpha 2 receptors
decrease in sympathetic outflow
decrease in insulin reelease
what are the four main functions of Beta 1 receptors
- increase in heart rate
- increase in contractility
- increase in renin release
- increase in lipolysis
what are the seven main functions of Beta 2 receptors
- vasodilation
- bronchodilation
- increased heart rate
- increased contractility
- increased lipolysis
- incrased insulin release
- decreased uterine tone
what does M1 receptors act on
CNS and enteric NS
what are the two functions of M2 receptors
decrease in heart rate and contractility of atria
What are the six major functions of M3 receptors
- increase in exocrine gland secretions
- increase in gut peristalsis
- increase in bladder contraction
- bronchoconstriction
-increase in pupillary sphincter muscle contraction
- ciliary muscle contraction
what are the major function of D1 receptors
- Relaxes renal vascular smooth muscle
what is the main function of D2 receptors
- modulates transmitter release especially in the brain
what are the four main functions of H1 receptors
- increase in nasal and bronchial mucus production
- contraction of bronchioles
- pruritus
- secretion
What is the main function of H2 receptors
increase gastric acid secretion
Wha tis the main function of V1 receptors
increase vascular smooth muscle contraction
what is the main function of V2 receptors
- Increase in H2O permeability and reabsorption in the collecting tubules of the Kidney
Wha tis the Gq receptor pathway
- Activation of phospholipase C
- Lipids are converted to PIP2
- PIP2 is converted to IP3 and DAG
- IP2 increase Calcium intake
- DAG activates protein kinase C
What is the Gs recptor pathway
-Activation of Adenylyl cyclase
- activation of ATP to cAMP
- cAMP activates protein Kinase C
What is the Gi receptor pathway
- activation of Adenylyl cyclase
- decrease in cAMP
- decrease in protein Kinase A
What drug blocks choline uptake by cholinergic neurons
= Hemicholinum
What block conversion of choline to ACh in the cholinergic neurons
- vesamicol
what blacks ACH vesicle binding in cholinergic receptors preventing its release
- botulinum
what blocks conversion of tyrosine to DOPA
metyrosine
what blocks uptake of norepi into vesicles in Noradrenergic neurons
Reserpine
what blocks NE vesicle binding in Noradrenergic neurons to prevent the release of NE
Guanethidine
what increases NE vesicle binding in noradrenergic neurons
amphetamine
what three things block NE reuptake by Noradrenergic receptors
- cocanine
- TCA's
- amphetamine
Bethanechol
direct cholinomimetic agent used for postoperative and neurogenic ileus and urinary retention
Resistant to AChE
what is the function of bethanechol
- activates bowel and bladder smooth muscle
resistant to AChE
Carbachol
Direct cholinomimetic agent used for the treatment of glaucoma, to promote pupillary contraction and relief of intraocular pressure
resistant to AChE
what does carbachol act similar to
acetylcholine
Pilocarpine
Direct cholinomimetic agent that is a potent stimulator of sweat, tears, and saliva
You cry, drool, and sweat on your PILlow
what are are the two main functionos pilocarpine
contacts ciliary muscle of eye and pupillary sphincter
what drug is used for the challenge test for diagnosis of asthma
methacholine
what is the action of methacoline
stimulates muscarinic receptors in airway when inhaled
what are the four main direct agonists for cholinomimetic agents
- Bethanechol
- Carbachol
- Pilocarpine
- Methacholine
what are the five indirect cholinomimetic agents
- neostigmine
- pyridostigmine
- Edrophonium
- Physostigmine
- Echothiophate
Neostimine
Indirect cholinomimetic agonist is used to treat postoperative and neuro genic ileus and urinary retetion, Myasthenia gravis, reversal of neuromuscular junction blockade
What is the action of neostigmine
Anticholinesterase inhibitor
increases indogenous ACh
what two anticholinesterases dont penetrate the CNS
- Neostigmine
- Pyridostigime
what are the two actions of pyridostigmine
- Anticholinesterase inhibitor
increase endogenous ACh
- Increase strength
what is the clinical application for Pyridostigime
Anticholinesterase inhibitor
long acting myasthenia gravis treatment. Increases endogenous ACh
pyRIDostigmine gets rid of MG
what drug is short acting for diagnosis of Myasthenia gravis
edrophonium
what is the main action for edrophonium
Anticholinesterase inhibitor
increases endogenous ACH
what drug is used to treat atropine OD and glaucoma
physostigmine Anticholinesterase inhibitor
can cross CNS
Chothiophate
Anticholinesterase used to treat glaucoma, increases endogenous ACh
what three things should be watched for with choliomimetic agents
- exacerbation of COPD, Asthma and peptic ulcers
what is the antidote for cholinesterase inhibitor poisoning
- atropine and pralidoxime
what drug regenerates active AChE
pralidoxime
what normally causes cholinesterase inhibitor poisoning
- organophosphates
what are the symptoms of cholinesterase inhibitor poisioning
D - Diarrhea
U - Urination
M - Miosis
B - Bronchospasm
B - Bradycardia
E - Excitation of Skeletal muscle and CNS
L - Lacrimation
S - Sweating
S - Salivation
what three muscarinic antagonists treat the eye
- atropine
- homatropine
- tropicamide
what is the function of muscarnic antagonists on the eye
produce mydriasis and cycloplegia
what two muscarinic antagonists treat the CNS
- Benztropine for Parkinson's and scopolamine for motion sickness
what muscarinic antagonist drug treats motion sickness
scopolamine
what muscarinic antagonist drug treates parkison's disease
Benztropine
what muscarnic antagonist is used to treat the respiratory system
Ipratropium
what is Ipratropium used to treat
- asthma and COPD
what two muscarinic antagonists treat the genitourinary tract
- ocybutynin
- glycopyrrolate
what is the function of oxybutynin and glycopyrrolate
- reduce urgency in mild cystitis and reduce bladder spasms
what three muscarinic antagonists are used for the GI tract
- methscopolamine
- pirenzepine
- propantheline
what are methscopolamine, pirenzepine and propantheline used to treat
- peptic ulcers
how does atropine affect the eye
increased pupil dilation and cycloplegia
how does atropine affect the airway
decreased secretions
how does atropine affect the stomach
decreased acid secreation
how does atropine affect the Gut
decreased motility
how does atropine affect the bladder
- decreaed urgency in cystitis
what are the the six main atributes of atropine toxicity
- increased temp due to decreased sweating
- rapid pulse
- dry mouth and skin
- cycloplegia
- constipation
- disorientation
what can atropine cause in elderly
acute angle closure glaucoma
what can atropine cause in men with prostatic hyperplasia
urinary retention
what can atropine cause in infants
hyperthermia
what is hexamethonium used for
-nicotinic receptor antagonist
ganglionic blocker to prevent vagal reflex responses to changes in blood pressure
- prevents reflex bradycardia caused by NE
- helps smokers quit
what are the four main atributes of hexamethonium toxicity
- severe orthostatic hypotension
- blurred vision
- constipation
- sexual dysfunction
what receptors does EPI act on
- alpha 1 and 2
- Beta 1 and 2
Beta 1 at low doses
Main treatment indications for epinephrine
anaphylaxis, open angle glaucoma, asthma, hypotension- increases HR and SBP while decreasing DBP resulting in a widening of pulse pressure
what receptors are targeted with NE
alpha 1, alpha 2 > Beta 1
what is NE used to treat
- hypotension increases both SBP and DBp so now pulse pressure widening, decreases HR
what drug is isolated to beta receptors
isoproternol
what is used to treat AV block
- Isoproterenol
what receptors are targets for dopamine
D1=D2 > B >alpha, requires increasing doses to get B and alpha
What is dopamine used to treat
shock by improving renal perfusion; inotropic and chronotropic for treating heart failure
Dobutamine
highest affinity for Beta1, used to treat heart failure, inotropic but not chronotropic, cardiac stress testing
what drug is used for cardiac stress testing
dobutamine
what receptors are targeted for dobutamine
B1 > B2, inotropic but not chronotropic
what sympathomimetic drug is used for pupillary dilation, vasoconstriction and nasal decongestion
- phenylephrine
what receptors are targeted with phenylephrine
alpha 1 > alpha 2
what two sympathomimetic drugs are used to treat acute asthma
- metaproterenol and albuterol
what drug beta agonist is used for long term treatment of asthma
salmeterol
what two drugs is used to reduce premature uterine contractions
terbutaline and ritodrine - target Beta2 receptors terbutaline also has B1
what are the four main beta2 agonists
- metaproterenol
- albuterol
- salmeterol
- terbutaline
Tyramine
indirect sympathomimetic, precursor for various sympathetic molecules, cleared by MAO, MAO-inhibitors can decrease clearance and cause HTN
what indirect sympathomimetic is used to treat narcolepsy, obesity and ADD
amphetamine - indirect general agonist, releases stored catecholamines
what indirect sympathomimetic is used to treat nasal decongestion, urinary incontinence and hypotension
- Ephedrine - indirect general sympathomimetic, releases stored catecholamines
what indirect sympathomimetic causes vasoconstriction and local anesthesia
cocaine - general agonist, uptake inhibitor
what are the three main indirect sympathomimetics
- Amphetamine
- Ephedrine
- Cocaine
what is the mechanism of action for amphetamiene
releases stored catecholamines
wha tis the mechanism of action for ephedrine
releases stored catecholamines
what is the mechanism of action for cocaine
uptake inhibitor
what are the two main sympathoplegics
- Clonidine
- Alpha-methyldopa
what is the mechanism for sympathoplegics
centrally acting alpha-2 agonists, decrease central adrenergic outflow
what is the application for sympathoplegics
- hypertension especially with renal disease because there is no decrease in blood flow to kidney
what drug is an irreversible non-selective alphablocker
- phenoxybenzamine, used to treat pheochromocytoma especially before tumor removal
SE: orthostatic hypoTN, reflex tachycardia
what drug is a reversible non-selective alphablocker
phentolamine; for patients on MAO-inhibitors who eat tyramine containing foods
what is the toxicity from non-selective alpha blockers
- orthostatic hypotension and reflex tachycardia
what are three alpha 1 selevtive blockers
- prazosin
- terazosin
- doxazosin
what are the mains uses of alpha 1 selective blockers
- hypertension
- urinary retention in BPH
what is the toxicity from alpha-1 selective blockers
- 1st dose hypotension
- dizziness
- headache
what drug is an alpha 2 selective blocker
Mirtazapine
what is mirtazapine used to treat
depression
what are toxicity symptoms from mirtazapine
- sedation
- increased serum cholesterol
- increased appetitie
what 6 applications are beta-blockers used for
- hypertension
- angina pectoris
- MI
- SVT
- CHF
- Glaucoma
what two drugs are used to treat SVT
- propranolol
- esmolol
what drug is used to treat glaucoma
- timolol
What is the effect of beta-blockers for hypertesnionj
- decrease Cardiac output
- decrease renin secretion
what are the effects of beta blockers for angina pectoris
- decrease heart rate and contractility resulting in decreased oxygen consumption
what is the effect of betablockers for MIs
decrease mortality
what is the effect of betablockers for SVT
decrease in AV conductioin velocity, class II antiarrhythmic
what is the effect of beta blockers for CHF
slows progression of chronic failure
what is the effect of timolol
decreases secretion of aqueous humor for the treatment of glaucoma
what are the four signs of beta-blocker toxicity
- impotence
- exacerbation of asthma-B1 selective prevents
- cardiovascular adverse effections
- CNS adverse affects
what are the four non-selective beta blocker antagonists
- propranolol
- timolol
- nadolol
- pindolol
Please Try Not being Picky
what are the five B1 selective antagonists
- acebutolol
- betaxolol
- Esmolol
- atenolol
- Metoprolol
A BEAM of beta-blockers
what are the two nonselective alpha and beta antagonists
- carvedilol
- labetalol
what are the two partial beta agonits
- pindolol
- acebutolol
what are Beta one selective antagonists useful for
- patients with comorbid pulmonary disease
what patients should beta-blocker use be cautioned for
diabetics
what are the three cardiac adverse affects from beta-blocker toxicity
- bradycardia
- AV block
- CHF
what are the CNS adverse effects from beta-blocker toxicity
- sedation
- sleep alterations
what is the treatment for acetaminophen toxicity
- N-acetylcysteine replenishes glutathione
what is the treatment for salicylates toxicity
- NaHCO3 (alalinize urine)
- dialysis
what is the treatment for Amphetamine toxicity
- NH4Cl (acidify urine)
what is the treatment for acetylcholinesterase inhibitor toxicity
- atropine and pralidoxime
what is the treatment for organophosphate toxicity
atropine and pralidoxime
what is the treatment for antimuscarnic toxicity
- physostigmine salicylate
what is the treatmenet for anticholinergic aget toxicity
- physostigmine salicylate
what is the treatment for beta-blocker toxicity
glucagon increases ionotropy and chronotropy of heart
what is the treatment for Digitalis toxicity
- stop dig, normalize K+, lidocane, anti-dig Fab fragments and magnesium (KLAM)
what is the treatment for iron poisining
deferoxamine
what are the four treatments for lead poisoining
- CaEDTA
- Dimercaprol
- succimer
- penicillamine
what are the two treatments for mercury, arsenic and gold poisoning
- dimercaprol (BAL)
- succimer
what is the treatment for copper, arsenic, gold poisoning
- penicillamine
wha tare the three treatments for cyanide poisining
- nitrite
- hydroxocobalamin
- thiosulfate
what iare the two treatments for methemoglobin toxicity
- methylene blue
- vitamin c
what is the treatment for carbon monoxide poisoning
- 100 percent O2 and hyperbaric oxygen
what are the three treatments for methanol, ethylene glycol posioning
- ethanol
- dialysis
- fomepizole is preferred
what is the treatment for opiod OD
Naloxone/naltrexone
what is the treatment for benzodiazepine OD
flumazenil
What is the treatment for TCA OD
NaHCO3 (plasma alkalinization)
what is the treatment for heparin OD
Protamine
what is the treatment for Warfarin OD
- vitamin K and fresh frozen plasma
what is the treatmetn for tPA and streptokinase toxicity
- Aminocaproic acid
what is the treatment for Theophylline posioning
B-blocker
What drug causes atropine like side effects
TCAs
what two drugs cause coronary vasospasm
- cocaine
- sumatriptan
what four drugs cause cutaneous flushing
- Vancomycine
- Adenosine
- Niacin
- Calcium channel blockers
VANC
What two drugs cause dilated cardiomyopathy
- Doxorubicin (Adriamycin)
- daunorubicin
what two drugs cause Torsades de pointes
- class three (sotalol)
- Class IA (quinidine) antiarrhymics
What six drugs can cause agranulocytosis
- clozapine
- carbamazepine
- colchicine
- propylthiouracil
- methimazole
- dapsone
what five drugs can cause aplastic anemia
- chloramphenicol
- benzene
- NSAIDs
- Propylthiouracil
- methimazole
what drug can cause direct Coombs-postive hemolytic anemia
methyldopa
What drug can cause gray baby syndrome
chloramephenicol
what six drugs can cause hemolysis is G6PD deficient pts
- Isoniazid (INH)
- Sulfonamides
- Primaquine
- Asprin
- Ibuprofen
- Nitrofurantonin
Hemolysis IS PAIN
what three drugs can cause megaloblastic anemia
- phenytoin
- methotrexate
- sulfa
Having a BLAST with PMS
what drugs cause thrombotic complication
OCPs especially in smokers
what drugs cause cough
- ACE inhibitors
what three drugs can cause pulmonary fibrosis
- Bleomycin
- Aminodaron
- Busulfan
what drug can cause acute cholestatic hepatitis
erythromycin
What six drugs can cause agranulocytosis
- clozapine
- carbamazepine
- colchicine
- propylthiouracil
- methimazole
- dapsone
what five drugs can cause aplastic anemia
- chloramphenicol
- benzene
- NSAIDs
- Propylthiouracil
- methimazole
What three drugs can cause focal to massive hepatic necrosis
- Halothane
- valproic acid
- Acetaminophen
What fungus can cause focal to massive hepatic necrosis
Amanita phalloides - amanitin
what drug can cause hepatitis
INH
What three drugs can cause pseudomembranous colitis
- Clindamycin
- Ampicillin
cephalosporins
what drug can cause adrenocortical insufficiency
Glucocorticoid withdrawal by HPA suppresion
what 6 drugs can cause gynecomastia
- Spironolactone
- Digitalis
- Cimetidine
- Chronic Alcohol Use
- estrogens
- Ketoconazole
Some Drugs Create Awesome Knockers
what two drugs can cause hot flashes
Tamoxifen
Clomiphene
what three drugs can cause hypothyroidism
- Lithium
- amiodarone
-sulfonamides
what drugs can cause gingival hyperplasia
phenytonin, verapamil
what two drugs can cause gout
- Furosemide
- thiazides
-niacin
-cyclosporine
-pyrazinamide
what two drugs can cause osteoporosis
- corticosteroids
- heparin
what three drugs can cause photsensitivity
- Sulfonamides
- Amiodarone
- Tetracycline
What 8 drugs can cause rash (stevens - Johnson syndrome)
- Ethosuximide
- Lamotrigine
- Carbamazepine
- phenobarbital
- phenytonin
- Sulfa drugs
- penicillin
- Allopurinol
bad rash after a PEC SLAPP
What four drugs can cause SLE-like syndrome
- Hydralazine
- INH
- Procainamide
- Phenytoin
what drugs can cause tendonitis, tendon rupture and cartilage damage in kids
- Fluoroquinolones
What drugs can cause fanconi's sydrome
- expired tetracycline
what three drugs can cause interstitial nephritis
- methicillin
- NSAIDs
- furosemide
What two drugs can cause hemorrhagic cystitis
- cyclophosphamide
- ifosfamide
how do you prevent hemorrhagic cystitis from ifosfamide
- coadministering with mesna
what two drugs can cause Cinchonism
- Quinidine and quinine
what two drugs can cause diabetes insipidus
- Lithium and demeclocycline
what three drugs can cause parkinson like syndrome
- antipsychotics
- reserpine
- metoclopramide
what four drugs can cause seizures
- Bupropion
- imipenem/cilastatin
- isoniazid
what drugs can cause tardive dyskinesia
- antipsychotics
what four drugs can cause disulfiram like reaction
- Metronidazole
- certain cephalosporins
- procarbazine
- 1st generation sulfonylureas

acute sensitivity to EtOH caused by a buildup of serum acetylaldehyde -> really bad hangover
what drugs can cause nephrotoxicity and neurotoxicity
- polymyxins
what four drugs can cause nephrotoxicity/ototoxicity
- Aminoglycosides
- Vancomycin
- Loop diuretics
- cisplatin
What are the 8 inducers of p-450
- Quinidine
- Barbiturate
- St. John's Wort
- Phenytonin
- Rifampin
- Griseofulvin
- Carbamazepine
- Griseofulvin
- Carbamazepine
- Chronic alcohol use
What are the 8 inhibitors of p-450
- HIV protease inhibitors
- Ketoconazole
- Erythromycin
- Grapefruit juice
- Acute alcohol use
- Sulfonamides
- Isoniazids
- Cimetidine
what can induce and inhibit different isoforms of p-450
- Quinidine
what does alcohol dehydrogenase convert ethylene glycol to
- Oxalic acid
What does oxalic acid cause
- Acidosis and nephrotoxicity
what does alcohol dehydrogenase convert methanol to
- formaldehyde and formic acid
what does formaldehyde and formic acid cause
- severe acidosis and retinal damage
what does acetaldehyde cause
- nausea
- vomiting
- headache
- hypotension
what blocks acetaldehyde dehydrogenase
Disulfiram
what is acetaldehyde dehydrogenase form
Acetic acid
what blocks alchol dehydrogenase formation of acetaldehyde
fomepizole
what are the three competitive substrates for ADH
- Ethylene glycol
- Methanol
- Ethanol
what does Alcohol metabolism deplete
NAD+
What is NAD+ needed for in the liver
fatty acid oxidation in the liver and conversion of pyruvate to lactate
what does does depletion of NAD+ cause in the liver
fatty liver and lactic acidosis
what is responsible for the glow seen in some individuals after drinking
- Polymorphism in the gene that codes for acetaldehyde dehydrogenase
what are the 9 main sulfa drugs
- Celecoxib
- furosemide
- probenecid
- thiazides
- TMP-SMX
- sulfasalazine
- Sulfonylureas
- Acetazolamide
- Sulfonamide antibiotics

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