Pharm-Exam 1

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Isoniazid

Back 1

anti tuberculosis drug
slow vs. rapid acylators factor must be considered here
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Autosomal recessive trait  ’d synthesis of n-acetyltransferase (45% of whites and blacks in U.S.)
Slow acetylators have 4 – 6 X blood concentration of a given dose compared to fast acetylators & longer half-life
Fast acetylator phenotype expressed in  90% Asians

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Colchicine

Back 2

binds tubulin and inhibits microtubule polymerization

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Warfarin

Back 3

S and R enantiomer S 4X as strong
acts on vitamin K epoxide reductase

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genetic variation and propanalol

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40% to 70% variability

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atropine

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contraindicated in narrow angle glaucoma

is an acetylcholine receptor blocker

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pKa aspirin

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3.5

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percent protonated

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100/1 = 99%
1000/1 99.9 %
10000/ 1 == 99.99%

When pH = pKa == 50/50 = or 1

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ionized form or lipid soluble form ?

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If pH < pKa  protonated

If pH > pKa  unprotonated

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Bicarb uses to treat drug overdoses

Back 9

for weak acids to ion trap and excrete
aspirin , barbituates

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enalapril

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an ACE inhibitor

an example showing that the drug conc as it relates effect is not linear

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verapomil

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anti-arrythythmic

40% bioavailability

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changing dosing

Back 12

D * CF / NF

(D * F / F )

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scopolamine

Back 13

transdermal patch for motion sickness
behind the ear

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binds acidic drugs

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albumin

aspirin , phenytoin

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binds basic drugs

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globulins , alpha-1 acid glycoprotein (AAG)

lidocaine, quinidine, propanaolol

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areas of the brain that don't have a tight BBB ?

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pituitary near the vomit center in the medulla

Front 17

where can barbituates be found after they hit their target organ ?

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fat

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how can one give anesthics to mom, and not have it affect the baby ?

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there is an equilibrium at the maternal blood and fetal capillaries

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total body water

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42 L
28 IC , 14 EC 10 - ISF 4 - plasma

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how do we terminate drug action ?

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metabolism and excretion
metabolism -- makes compound more polar and makes it more soluble -- this also aids in excretetion

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steps in biotransformation

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phase I -- makes it more polar
phase II--conjugate to an endogenous subsrate (like glucuronic acid, sulfuric acid, acetic acid, amino acids) and make even more polar

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types of phase I reactions ?

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Oxidation
reduction
deamination
hydrolysis

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omeprazole

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inhibits 3 CYP isozymes responsible for warfarin metabolism

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****P450 1A2 inducers and sustrate
TWA

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s: theophylline (anti-asthma), warfarin
i :
Carbamazepine
Phenobarbitol

smoking, charcoal broiled foods, cruciferous vegie, omeprazole (ppi)

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****P 450 1A2 inhibitors
TWA

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Cimetidine (H-2 recep. antagonist)
Grapefruit juice
Erythromycin

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pseudocholinesterase

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Pseudocholinesterase deficiency is an inherited blood plasma enzyme abnormality. People who have this abnormality may be sensitive to certain anesthetic drugs, including the muscle relaxants succinylcholine and mivacurium as well as other ester local anesthetics.[1] Exhaustive list of drugs to avoid listed in following section. These drugs are normally metabolized by the pseudocholinesterase enzyme.

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first order kinetics

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% of total drug that is eliminated in a given time is constant.
morphine

When [drug] is high  rate of elimination is rapid
When [drug] is low  rate of elimination is slow

can be described by biologic half-life (T1/2).

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zero order kinetics

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EtOH

- constant amount is lost per unit time

for some drugs (ETOH, aspirin, phenytoin)
Drugs that saturate routes of elimination will disappear from plasma in a nonconcentration-dependent manner, which is zero-order.

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loading dose

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Loading Dose = Vd x CT/ F

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when you you give a loading dose ?

when/ what drug not for a loading dose ?

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a. digoxin (7 day half-life)

b. lidocaine, theophyline

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propanalol

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competetive antagonist to norepinephrine

used to lower force of contraction , BUT during activities where this is released , can overcome the propanalol .....

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clonidine withdrawl

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alpha-2 agonist activity reduces BP --withdrawl from , can prodice hypertensive crisis ----b/c the drug down-regulates alpha-2 receptors

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H1 receptor

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Fexofenadine/allegra

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5HT2 receptor

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Ketanserin

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NR3C2 receptor

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aldosterone

spironolactone

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neurotraqnsmitters
alpha1 receptor

B1, Beta2 rec.

Back 36

terazosin

metoprolol

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acetylcholinesterase drug

Back 37

edrophonium

Front 38

ACE

Back 38

Captopril

Front 39

Viamin K epoxide reductase

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warfarin

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dihydrofolate reductase

Back 40

methotrxate

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reverse transcriptase

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Zalcitabine, Dedanosine and Stavudine

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therapeutic index TI

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LD50/ ED 50
wide index is safer
close index means that the dose that saves and the dose that kills are very close

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partial agonists

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Stabilizes the a receptor equally in the active and in the inactive conformation
Pindolol, Carteolol @  receptors
Clozepine @ 5HT1A

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terazosin

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a competetive antagonist

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phenoxybenzamine

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non-competetive antagonist

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inverse agonist

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Possible when receptor has intrinsic activity
Second generation H1 blockers (fexofenadine)

reversing the number of receptors in the absence of bound ligand

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chemical antagonism

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In this type of antagonism, the antagonist can chemically interact with the agonist thereby making the agonist unavailable (e.g. protamine +ve, is a chemical antagonist to heparin)

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Gs

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Glucagon, Hist, Serotonin, catecholamines

effects - stim adenylyl cyclase , increases cAMP

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Gi1, Gi2, Gi3

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ligands : alpha-2 adrenergic amines, acetylcholine, opiods, serotonin

decreases adenylyl cyclase , decreases cGMP , opens K+ channels, decreases HR

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Gq

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ligand :
Bombesin, Serotonin (5HT1c) etc

effects: Phospholipase C up, IP3, diacylglycerol, cytoplasmic Ca 2+

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Gt1, Gt2

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Photons (rhodopsin and color opsins in retinal rod and cone cells)

effects:
inc. cGMP phosphodiesterase cGMP (photo transduction

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desensitization

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built in over flow check to prevent excessive stimulation of a receptor system. seen in G protein systems commonly.

GRK - Beta-arrestin pathway triggered --- GRK --causes phosphrylation to -O group , and B-arrestin binds there

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example of down regulated receptor ?

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EGF
epidermal growth factor
Mm --- when binding of an agonist to a receptor induces accelerated endocytosis

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phosphodiesterase inhibitors

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caffeine
theophylinne - used to treat asthma ---

G protein pathway

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cGMP pathway

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PDE here is inhibited by viagra

this also plays a role in altitude sickness

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significance of reversible phosphorylation

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signal amplification and flexible regulation

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imatinib, and trastuzumab

(nib and mab)

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Flexible Regulation: Protein kinases associated with phosphorylation in various second messenger pathways provide targets for drug therapeutics

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Maintainance dose

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clearance * SS Conc. (same as target conc)

(maintain with C's )

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nonlinear pharmacokinetcs

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serum drug conc. does not change proportionally with dose amount

ex: phenytoin (anti-epileptic)
theophyllin (anti-ashtma)
valproic acid, disopyramide

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what type of drugs would be part of the one compartment model ?

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polar drugs such as aminoglycosides

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some drugs are not distrubuted to "one compartment"

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dig, vanco

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you decide that TDM (therapeutic drug monitoring ) is a good idea , for a drug with a narrow TI , so you draw blood , when should this be done ?

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plasma conc of the drug should be taken during steady state

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so, you do TDM for Theophyline , and find that the conc is 12 mg/ mL , within the range it should be , what is your clinical interpreation ?

Back 63

depends on how the patient is responding !!

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Drugs commonly monitored with peaks and troughs

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Gentamicin, Amikacin , Vanco
(GAV) like gavel

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loading dose

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Vd * C SS / F

or CSS - C observed * Vd / F

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neurotransmiter relased at muscurinic receptors ?

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Ach

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nt released at adrenergic receptors in symp. nervous system ?

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NorEpi

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neuroendocrine cells

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Nicotinic receptors synapse

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VMAT

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vescicular monoamine transporter

Front 70

enzymne that breaks down catecholamines ?

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found in the liver
COMT
catechol-O-methyl transferase

Front 71

alpha 1 receptor effects ?

Back 71

contraction of vascular smooth muscle as well as genitourinary smooth muscle

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alpha 2receptor effects ?

Back 72

pancreas, decrease insulin production
nerve , dec. norepi release

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Beta 1 stim

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increase contractility of the heart
increased conduction velocity of the heart
**also increases renin secretion

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beta-2 stim

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relaxation of smooth muscle

liverfunction

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connection btw Beta and Alpha 2
second messengers

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stim a beta rector and Gs is stim , increases cAMP
stim an alpha-2 -- and Gi is activated and cAMP levels drop

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alpha-1 second messages

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Gq, Dad , IP3, phopholipase C pathway

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effects of ephedrine ?

Back 77

promotes the release of norepi

amphetamines do the same

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what do you not do with Beta- blockers ? *****

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do not want to discontinue them suddenly. why ? when you block them , the body makes more .... if you stop blocking , then ... patient could exp. cardiac rebound excitation

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when can beta-2 blockers be bad ?

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with diabetics , why ?
masks tachycardia indicitative of hypoglycemia in diabrtics

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do catecholamines cross BBB ?

Back 80

no, polar!! so minimal effects on CNS
can't use orally!! MAO in liver breaks it down

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likes alpha 1 more than 2

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phenylephrine, methoxoamine

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likes alpha 2 more than 1

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clonidine

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likes B1 more than B2

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NorEpi

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likes B1 more than B2

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Dobutamine

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likes Beta 2, more than 1

Back 85

albuterol, ritodrine, terbutaline, metaproterenol

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alpha-1 agonsits

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phenylephrine --nasal spray

long acting - ephedrine, pseudoephedrine

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Mydriasis

Back 87

dilated pupils
facilitated by phenylephrine for retinal exams

Front 88

how does stim alpha-2 lower BP and HR ?

Back 88

it decreases norepi release!!!

Front 89

name and type of drugs used to delay premature labor ?

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beta agonsts

terbutaline, ritodrine

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rebound hypertension caution with ?

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alpha-2 receptors

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adverse effects of alpha-1 agonists

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tissue necrosis , hypertension

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alpha-1 agonisits

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PEP

Phenylephrin, ephedrine, psuedoephedrine

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alpha-2 agonists

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clonidine

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dopamine receptor

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dilates renal blood vessels (D1)

higher doses activate cardiac B1 and inc. cardiac perfromance --shock treatment

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D1 selective agonist

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Fenoldopam

Front 96

indirect acting sympathomimetics

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Tyramin
if taking a MAO , and taking in lots of amines in diet --get a release of NE

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alpha-blockers (non-selective)

Back 97

phentolamine, phenoxybenzamine
prevent acute hypertensiveepisodes due to excess catecholamine releae

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alpha-1 selective

Back 98

prazosin
used for hypeetension , BPH
Mm- dec. sympathetic tone of blood vessels

CAUTION!! decreased BP --can lead to reflex tachycardia and inc. CO

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adverse effects of alpha-1 blockage

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orthostatic hypotension
when patient stands up , there is a decreased venous tone (because there are alpha-1 receptors on the veins also, that are not vaso-constricting!!) venous return to the heart is dec. , CO is lowered, BP is lowered

Front 100

blocking alpha-2 adverse effects ?

Back 100

well, not inhibitin NE release

Front 101

Beta-blockers

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effects due to cardiac B1 blocker

dec HR , force of contraction , dec conduction through the AV node

indications :
angina, hypertension , arrhymias , MI

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propanolol

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non-selective Beta-blocker

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cardio-selective Beta -1

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metoprolol

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adverse effects of Beta-1 blockage

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rebound cardiac excitation if discontinued suddenly , b/c receptors are up-regulated
sudden termination can lead to sudden death

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indirect acting sympatholytics

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Reserpine --irreversible damage to VMAT
Tyramine

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Bethanechol

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stimulates an atonic bladder --used in urology

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Pilocarpine

Back 107

ophthalmology
used for emergency lowering of intraocular pressure

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Muscarinic antagonists

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Atropine
Scopolamine
Tropicamide
Ipatropium, Tiotropium

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Ipatopium

Back 109

syn analog of atropine
use as an inhaled drug for asthma and COPD

bocks Ach at M receptors in lungs -aerosol

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Tiotropium

Back 110

longe bronchodilator activity

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cycloplegia

Back 111

relaxation/ paralysis of ciliary muscles

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atropine and scopolamine used for ..

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mydriasis (blocks iris sphincter muscles)
cycloplegia (relaxation/paralysis of ciliary muscle)
Both facilitate opthalmoscopic examination

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adverse effects of atropine

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dry mouth , dry eyes , blurred vision , can't sweat

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atropine toxicity

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dry as a bone , blind as a bat , red as a beet , mad as a hatter , hot as a hare

(blocking sweating and salivation)

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reversible cholinesteras inhibitors

Back 115

Neostigmine
Physostigmine
Edrophonium
Pyridostigmine

Front 116

Ach-esterase inhibitors --clinical apps

Back 116

1. atropine intox give
physostigmine
2. for MG , give edrophonium, pyridostigmine

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irreversible Ach-I

Back 117

Echothiophate
Sarin
Malathion

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M3 receptors

Back 118

in smooth muscle and and glandular tissue
phospholipase C -IP3- mobilizes internal Calcium and DAG cascade

Front 119

location of M2 receptors ?

Back 119

heart
decreases adenylyl cyclase just as alpha-2

Front 120

stim M receptors in the eye

Back 120

contraction and miosis

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ciliary muscle

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contraction and accomadation for near vision

Front 122

stimulate salivary and lacrimal glands

Back 122

thin and watery secretions

Front 123

high doses of muscarinic agonsits, affects on the heart ? what is the primary concern ?

Back 123

AV block

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Bethanocol

Back 124

used in urology , stim an atonic bladder (ie -relaxed )

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Pilocarpine

Back 125

opthomology --used for emergecny lowering of intraocular pressure

Front 126

when would you use a muscarinic agonist ?

Back 126

to void the bladder, as well as to lower intra-ocular pressure

Front 127

muscarinic antagonists

Back 127

atropine , scopolamine, tropicaminde , Ipatropium, Tiotropium

Front 128

Muscarinic receptors in diff organs are not equally sensitive to muscarinic blockage

Back 128

salivary glands , sweat glands bronchial glands -- most sensitive

stomach , lung dilation least sensitive

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Tropincamide

Back 129

shorter acting Mus. blocker

Front 130

Ipatropium , and Tiotropium

Back 130

analogues of atropine
used for asthma treatment

Tiotropium --longer acting

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hot as a hare

Back 131

atropine toxicity
body temp rises, why ? can't sweat for one ...

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pralidoxime

Back 132

cholenesterase reactivator (2-PAM)
binds to the inhibitor and displaces it

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ganglionic blocker

Back 133

competietively block Ach at Nicotinic receptors , shuts down entire ANS

Front 134

Mecamylamine and Trimethaphan(IV
only)

class and use ?

Back 134

ganglionic blockers

sometimes used to produce controlled hypotension during neurosurgery --there are better agents available now