Pat Hop Harm Exam 3 Drugs

8/2/2019 Pat Hop Harm Exam 3 Drugs

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Categories Class Individual drugs MOA Coverage

amoxicillingm pos, Strep and

Staph

1st-cephalothin gram pos

2nd-Cefamandolegram pos & some

gram neg

3rd-Cefotaximegram pos & some

gram neg

4th-Cefepimegram pos & best for

gram neg

Pyrazinamide

erthromycin

clarithromycin

azithromycin

Isoniazid

Prevents

elongation of

peptide chain at

30S ribosomalsubunit

broad spectrum but

resistance

developed in many

species

Ethambutol

Macrolides

Antibiotics

Inhibitors of Protein

(Bacteriostatic)

Inhibits Bacterial Cell WallSynthesis (Myobacteria)

gram pos aerobes &

Beta Lactams- Inhibits

Bacterial Cell Wall Synthesis

ampicillin,piperacillin

few gm neg -

Neisseria gn,syphillis, some

anaerobes

gram pos & some

gram neg

Tuberculosis Drugstarget Myobacteria

Prevents

elongation of

peptide chain at

50S ribosomal

Inhibits formation ofcell wall Acid-fast bacilli

Disrupts cell wall

synthesis (kills cell

by osmotic

pressure) Not

effective against

most Gram

negative

cephalosporins

Carbapenems imipenem,meropenem,

ertapenem

Extremely Broad

Spectrum! grampos, gram neg,

anaerobes

Penicillin

Non-Beta Lactams- Inhibits

Bacterial Cell Wall Synthesisvancomycin Vancomycin gram pos

Tetracylines

tetracyline,

doxycycline,

minoclycline

Rifampin


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??? MetronidazoleMetronidazole

(Flagyl)???

Anaerobes,

parasites & bacteria

Inhibits Enzymes important in

microoganism's functionFluoroquinones

Ciprofloxacin,

levofloxacin,

oxofloxacin

Inhibits enzyme(DNA gyrase) that

is important in DNA

replication

Aerobic, most gram

neg and gram pos

Inhibits Nucleic Acid

Synthesis

Sulfamethoxazole-

trimethroprim

(Bactrim)

Sulfamethoxazole-

trimethroprim

(Bactrim)

Blocks bacterial

enzymes important

in the synthesis of

DNA, RNA, and

proteins

Broad Spectrum-

gram pos & gram

neg

AminoglycosidesGentamycin,tobramycin,

amakacin

Bind to30S

ribosome and

promote theformation of

abnormal proteins

(killing cell)

gram neg, Noactivity against

anaerobes

anaerobes

Inhibits Protein Synthesis(Bacteriocidal)


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KetoconazoleInhibits synthesis of

sterol componentsystemic infections

Acyclovir;

Valcyclovir (Valtrex)

is prodrug

suppresses

synthesis of Viral

DNA

all herpes viruses

ganciclovirall herpes viruses,

CMV

Influenza Drugs

amantadine,rimantadine

only for Influenza A

oseltamivir (tamiflu);

zanamivir (Relenza)

prophylaxis

(Tamiflu) or to

shorten flu (both)

HIV Drugs

Nucleoside Reverse

Transcriptase Inhibitors (NRTI)Zidovudine (AZT)

Inhibit viral enzyme

(reverse

transcriptase) that

converts RNA to

DNA by terminating

DNA strand

Protease Inhibitors (PI)Indinavir, ritonavir,

saquinavir, etc

Inhibits viral

protease so virus

doesn't mature

Entry Inhibitors (prevent entry

of HIV into CD4 cells)

Fusion Inhibitors Enfuvirtide

Non-Nucleoside Reverse

Transcriptase Inhibitors

(NNRTI)

Nevirapine,

delavirdine,

efavirenz

Binds to ative site

on reverse

transcriptase

HIV

Attachment

Inhibitors

Maraviroc

(Selzentry)

CCR5antagonist so

HIV doesn't attach

to CD4 cell (MCII)HIV

Binds to gp41, viral

envelope protein

Antifungals

Amphotericin B

Binds to sterols to

permeability (cell

bursts)

systemic infections

Antivirals


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Diuretics

Thiazide Diureticshydrochlorthiazide,

chlorthalidone

prevent

reabsorption of Na

in distal tubule

1st line use in HTN;

edema

Loop Diuretics Furosemide (Lasix)

prevent

reabsorption of Na

in ascekding Loop

of Henle

2nd line HTN;

pulmonary edema

assoc. w/CHF;

edema of hepatic,

cardiac or renal

origin

Potassium Sparing

Diruetics

Sironolactone

(Aldactone)

prevent

reabsoprtion of Na

from collecting

tubule and duct

HTN, edema, in

combo w/Loop or

thiazide diuretics

Triamterenegiven combo

w/thiazide

Osmotic Diuretics Mannitol (sugar)

prevents H2O

reabsorption fromproximal tubule

prophylaxis of renal

failure, reduceintracranial pressure

Integrase Inhibitors Raltegravir

Blocks integrase

enzyme to prevent

viral genetic

information from

integrating w/ hostcell DNA


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Drugs Acting on the

RAAS

Renin Inhibitors aliskiren (Tekturna)

inhibits conversion

of Renin to

Angiotensin I tostop RAAS

monotherapy or

combo w/thiazide

ACE inhibitorcaptopril, lisinopril,

enalapril

inhibits Angiotensin

Converting Enzyme

from Converting

Angiotensin I to II

HTN, Heart failure,

diabetic

nephorpathy, post

MI prophylaxis,

prevention of MI,

stroke

ARBblocks release of

Aldosterone

similar to ACEI plus

stroke prevention

Aldosterone

Antagonists

spironolactone,

epleronone

K-sparing diuretics

block Aldosterone;promote Na and

H2O excretion in

collecting tubule

and duct

Sympatholytics

Beta-blockers

block beta 1 and

beta 2 receptors;

some 'partial'

agonists= block NE

binding but activate

a little bit

HTN

acebutolol (ISA),

atenolol, esmolol,

metolprolol

cardioselective

beta 1 blockers

HTN, some angina,

dysrhythmias, MI

pindolol (ISA),

propranolol

nonselective beta

blockers

HTN; angina,

dysrhythmias, MI,

migraine

(propranolol)

carvedilol, labetololnonselective

alpha/beta blockersHTN

Alpha-1 Antagonistsdoxazosin,

terazosin, prazosin

block alpha-1

receptors in

arterioles andveins= dec.

peripheral

resistance and

venous return to

heart

HTN- not 1st line

use


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Centrally acting

Alpha-2 agonists

clonidine,

methyldopa

act in brainstem to

suppress

sympathetic

outflow to heart=

dec. BP and COClacium channel

blockers

Dihydropyridinesnifedipine,

amlodipine

block Ca channels

in arterioles

angina, HTN

Nifedipine=

sustained release;

Amlodipine= longer

t1/2, no sustained

release

Non-dihydropydrinesVerapamil,

diltiazem

block Ca channels

in arterioles and

heart

angina, HTN,

dysrhythmias

Drugs for Hypertensive

Emergency

Sodium

notroprusside

(Nitropress)

powerful

vasodilator

HTN emergency-impending end-

organ damage

(about to have

stroke)

Calcium channel

blockers

fenoldepam,

nicardipine,

clevidipine,

diltiazem

HTN emergency

Lipid Lowering Drugs

Statins

atorvastatin

(Lipitor), fluvastatin,lovastatin

inc. LDL receptros,

reduce cholestrolsynthesis in liver

hypercholesterolemi

a; prevention of MI,stroke, angina;

Diabetes

Bile Acid

sequestrants

cholestyramine,

colestopol,

colesecelam

Decr. Bile acid

reabsorption= incr

synthesis in liver=

incr. need for

cholesterol= incr.

LDL receptors

reduced LDL,

usually used

w/Statin


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Cholesterol

Absorption Inhibitors Ezetimibe (Zetia)

acts on cells in

brush border of SI

to inhibit

cholesterol

absorption; blocksabsorption of

dietary cholesterol

& cholesterol

secreted in bile

lowers LDL & TG,

raises HDLs

Nicotinic Acid

(Niacin)

reduceds TG &

LDL; raises HDL

used to lower TG

levels in pt

w/pancreatitis

Fibric Acid

derivatives

(Fibrates)

gemfibroil,

fenofibrate (Tricor)

incr. lipoprotein

lipase= lower

VLDLs & incr. TG

storage (decr. TG

in serum); raisesHDL; no effect on

LDL


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CSF

penetratio

n

Adverse Effects and Drug

InteractionsMisc. Misc continued/ Interactions

Reserve for serious infections

Charged drug= not absorbed; IV or

topical use; single or daily dose

divided b/c kills bacteria even afterblood levels decline

Low levels between daily dose

allow for washout from body cells

to prevent toxicity

Hypersensitivity, blood dyscrasiascombo sulfa drug & inhibitor of

bacterial enzyme

Stephen-JohnsonUsed for UTI, prophylactically, and

pneumonia of AIDS

kidney-bladder stones remain well hydrated

CNS effects

Increase Warfarin and theophylline(bleeding) Don't take w/ aluminum, iron,calcium, or zinc (no Tums)

irreversible joint disease


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CSF

penetratio

n



Toxic to Mammalian cells b/c of

cholestrol in membrane;AMPHOTERRIBLE!!!

Phlebitis; Use Topical Instead

nephrotoxicity

Strong Inhibitor of cytochrome P450 Can be used topically rare hepatic necrosis

nephrotoxic;

immuization for chicken

pox/shingles available- caused by

Herpes Zoster

resistance due to thymidine kinase

deficiency

granulocytopenia, thrombocytopenia;

teratogenic, embryotoxic

only used for CMV in

immunocompromised pt; excreted

unchanged in urine

prophylaxis during epidemics andas tx

resistance may be problem

oral only (Tamiflu); inhaled

(Relenza); must be taken very

soon after 1st symptoms

Mitochondrial toxicity in liver, lactic

acidosis, bone marrow depression,

GI toxicity, inhibit Human DNA

polymerases (toxic to dividing cells)

peripheral lipoatrtophy (esp. d4t),

peripheral neuropathy

Treat w/ combination (ART, ARV,

HAART)

cP450 interactions (nevirapine

induces; others inhibit)Doesn't effect human DNA NO skipping doses

Steven-Johnson, hepatotoxicity Bad side effectshyperglycemia, fat redistribution,

hyperlipidemia, bleeding in

hemophilla, osteoporosis, liver

enzymes, ECG changes (prolonged

QT), GI effects, ALL METABOLIZED

by cP450

Despite bad effects they are so

important that they are rarely d/c

Wait til CD4+ drop below a certain

level

gp41 mutates so drug can't bind=

resistance

Treat w/ combination (ART, ARV,

HAART)Extremely expensive

subQ 2x/day

limited supply NO skipping doses

reserved for those who failed other

tx

Cough, fever, muscle & joint pain,

liver toxicity, stomach pain

Bad side effects; must have genetic

testing

Careful w/ ppl w/ cardiovascular

disease

Only works for CCR5 receptors

injection site reactions; risk of

pneumonia increased


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CSF

penetratio

n



x2 daily = compliance issueWait til CD4+ drop below a certain

level

1 opportunity for this to beeffective, once genetic information

is incorportated it is too late

plasma concentrations reduced byenzyme inducers= rifampin

HYPOkalemia, hyponatremia,

hypochloremia, dehydration;

orthostatic hypotention

Interactions: Digoxin toxicity; Lithium

toxicity; no NSAIDS

same as Thiazides; ototoxicitypromotes diuresis in renal

impairment

Interactions: Lithium toxicity; Digoxin

can increase hypokalemia; other

ototoxic drugs, NSAIDS

HYPERkalemia (avoid K

supplements; synergistic w/ACE

inhibitors & ARB; Pregnancy cat D

due to steroid effects on fetus

can activate steroid receptors to

cause endocrine effects=

impotence, hirsutism,

gynecomastia

Interactions: ACE inhibitors and

ARBs may increase hyperkalemia;

potassium supplements and salt

substitutes contraindicated. Delayed

effects; if used w/Thiazide, K levels

may even out;

HYPERkalemia

Interactions: ACE inhibitors, ARBs,

NSAIDS, avoid K rich diet. Take

after meals A.M.

yes

edema (caution in CHF b/c blood

volume may overload heart);dehydration, orthostatic hypotension

must be given IV; increases

osmotic pressure of blood to drawedema fluid into vasculature

Interactions: not metabolized, veryinert; no significant interactions

diarrhea, nausea, headache


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CSF

penetratio

n



cough (bradykinin), angioedema

(bradykinin), teratogenic, may

precipitate acute renal failure, 1st

dose hypotension

hyperkalemia, dec. remodeling,

dec. blood volume, increase

bradykinin, dec. CV mortality from

HF, dec. renal failure in diabetics

Interactions: digoxin, Lithium, K

sparing drugs, K supplements. All

oral but enalaprilat IV only.

No cough; angioedema, renal failure

Interactions: hypotensive w/other

antiHTN drugs; kyperkalemia

w/other K-sparing diuretics

reduce HR, contractility, peripheral

resistance, and vasoconstriction;

suppress reflex tachycardia,

decrease Renin release

can also block Ca entry into cells;

ionotrope, dromotrope, chromotrope

ISA= intrinsic sympathomimetic

activity; partial agonists

orthostatic hypotension; sexual side

effects


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CSF

penetratio

n



dry mouth, sedation, hemolytic

anemia, liver disorders (bad side

effects!)

methyldopa OK for pregnancy;

rebound HTN if stopped abruptly

lower BP

stimulates

barorecepto

r refles to

incr. SNS to

stimulate

Beta

receptors in

heart= incr.HR &

contractility

flushing, dizzy, headache, edema;

gingival hyperplasin, constipation,

reflex tachycardia (give w/Beta

blocker)

dilates peripheral vessels = dec.

BP; dilates coronary arteries= inc.

coronary perfusion

all end in "-pine"; does NOT block

cardiac Ca channels

constipation, dizziness, facial

flushing, headache, edema,

bradycardia, conduction defects

Dilates periph. Blood vessels &

coronary arteries; blockade at SA,

AV nodes and myocardium= dec.

BP, HR, conduction and contractile

force, inc. coronary perfusion

cyanide poisoning; thiocyanate

toxicity >3 days (CNS effects)

no reflex tachycardia; short t1/2;

titrate to BP; use infusion pump

overshoot hypotension possible- can

be corrected fast

reflex tachycardia, hypotensionclevidipine, diltiazem easiest to

titrate/adjust due to short t1/2

myopathy, rhabdomyolysis,hepatotoxicity

Interactions: fibrates & ezetimibe=

incr. risk of myopathy; CP450

inhibitors (erythromycin,ketoconazole)incr. risk adverse

effects

lower LDL, TG; raise HDL; decr.

Inflammation & risk of thrombosis;

incr. endothelial cell function &vasodilation; increase osteoblasts;

Reverse effects of plaque

inert, can't

be

absorbed,

pass

through SI

& excreted

in feces

No systemic effects; GI symptoms

(except Colesevelam)= constipation,

bloating, nausea

Decrease absorption of: warfarin,

thiazides, digosin, iron, B blockers,

corticosteroids, Fat soluble

vitamins

prevents bile acids from being

reabsorbed in SI; excreted in feces;

reduce LDL, incr LDL receptors


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CSF

penetratio

n



taken w/Statins= risk of liver

damage; w/Fibrates= increase

concentration of cholesterol in bile

& risk of gallstones;

w/Cyclosporine= inhibitsmetabolism & incr. concentration;

Bile Acid sequestrants impair

absorption

keeps bile from entering body from

the diet; used w/Simvastin canincrease plaque

intense flushing, worse w/aspirin; GI

upset; hepatotoxic; hyperglycemia;

raises levels of homocysteine (may

incr. CV risk)

triple therapy (statin, Niacin, bile

acid sequestrant) = 70% lower LDLB vitamin at high dose

gallstones; myopathy; hepatotoxicity;

overlapping adverse effects w/statin

so use together with caution

interactions: warfarin=gemfibrozil

displaces from protein binding sites

to incr. efficacy; statins= incr. riskmyopathy

don't use w/Statins


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Pat Hop Harm Exam 3 Drugs

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