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Drugs Pharmacology

Drugs Pharmacology

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Anti Hypertensive Drugs
Name
MOA
Pharmacology
Toxicities/SDFX
Reflex
Contraindications
Administration Misc
Brain
DM, Hypokalemia
Loop (Furosemide/Lasix)
DM, Hypokalemia
RAAS Ihibiting Drugs
Name
MOA
Pharmacology
Toxicities/SDFX
Reflex
Contraindications
Administration Misc
w NSAIDS = HTN
Diuretics - DOC x HTN monotherapy
↓ plasma volume ECFV → ↓ VR → ↓ CO → ↓ MAP/BP → ↑ TPR (Reflex) → ↑ PRA → ↑ CO → a maintained lowered TPR; 1) ↓ intravascular volume and 2) ↓ vascula
responsiveness by ↓ Na and ↓ Ca++
Drug Drug
Interactions

Thiazides
(Hydrochlorothiazide/Hy
droDiuril/H2TZ)

Work on Distal
convoluted Tubule
(descending loop of
Henle?)

Sexual Dysfunction,

hypovolemia,
Hypokalemia/alkalosis,
Hypomanesemia,
Hypercalcemia,
Hyperuricemia,
Hyperlipidemia,
Hyperglycemia

w Quinidine=Torsade de
Pointes; w Digoxin= Dig

Toxicity; w
Cotricosteroids= Na
Retention; w Li= Plasma
[Li]; w Warfarin=
effectiveness; w
NSAIDS=HTN

Elderly or dehydrated or
other RxRx interactions;
DM, Hypokakemia

may need K
supplements; ↓ in K
→ ↓ BP and ↑
arrythmias

Along w tx HTN
Diuretics (in
general) are good
for Edema,
Dyspnea; Thiazides
are good x Severe
Renal Impairment w
HTN

Thiazide-like
(Chlorthalidone/Hygroton
)

blocks Na/2Cl-/K on
Ascending Loop of Henle
so they stay in lumen

Hearing Loss (just like
aminoglycosides),
Hypocalcemia

good x tx of HTN w
Renal Impairment
even morese than
Thiazides

K-Sparring
(Spironolactone,
Eplerenone/inspra)

Aldosterone receptor
antagonist; Reduce
aldosterone levels?

Estrogenid
SDFX/Gynecomastia b/c
of steroid like sx of drug;

NSAIDS, β blockers and
ACE inhibitors ↑
Hyperkalemia; may lead
to cardiac arrest

good x tx of HTN w
Hypkalemia
Drug Drug
Interactions
ACE Inibitors (end in -pril
eg Captopril)

Block A I: A II conversion
in lung endothelial cells;
↑ Bradykinin

↓ A-II prodx → ↓ TPR
and ↓ aldosterone and ↑
Na excretion; ACE
breaks down bradykinin,
so if it's blocked the
bradykinin can stick
around longer

Captorpril causes rash;
hpotension, Na
depletion; Dry cough →

↓ compliance,
Hyperkalemia bc K not

excreted bc aldosterone
is inhibited; Angioedema
(esp if black); Renal
Failure due to ↑ GFR,
Proteinuria, rashes
(captopril) fever,
pancytopenia, BM
depression

Great Results If
Used w Thiazides

Little sex dysfx
SDFX; help
manage DM;

mortality if prior
MI;o nly
antihypertensive mx
w/o sexual dysfx

Angiotensin II Receptor
Blockers/ARB's (end in "-
sartan"; Losartan,
Valsartan, Irbersartan,
Candesartan,
Telmisartan, Eprosartan)

Block AII type I receptors
→ ↓ aldosterone
relaease and vaeesel
relaxation

↑ bradykinin →
angioedema

Aldosterone Receptor
Blocker (Spironolactone,
Eplerenone)

Sympathoplegic Agents
CNS α2 Agonists; Ganglionic Blockers; Neurotransmitter Depletors; α, β, Blockers
Name
MOA
Pharmacology
Toxicities/SDFX
Reflex
Contraindications
Administration Misc
↓ HR, VR, TPR, CF
none :)
↓ HR, VR, TPR, CF
β blocker-Labetolol
β1, β2, α1 blocker
no reflex tachycardia
DM, Asthma, CHF
Angina
Ca++ Channel Blockers
Drug Drug
Interactions
α2 Agonists (Clonidine,
Guanabenz)

some orthostatic
hypotension; Dry Mouth,
Drowsiness, Depression;
Sexual Dysfx; Withdrawl
Supersensitivity;
Pseudotolerance

Ganglionic Blockers
(Trimthapham
Camsylate)

Orthostatic
Hypotension; Sexual

Dysfx; Paralytic Ileus,
Urinary Retention (esp
old men)

Vasodilation w/o
reflexes (cool)

Sympatholytic Agents
(Reserpine,
Guanethidine,
Guanadrel)

Deplete adrenergic
neurotransmitters
Reserpine: Suicide,
depression, ↓
sypmathetic action.

Guanethidine:
Retrograde
Ejaculation. Orthostatic

Hypotension, Fluid
Retention, Sexual Dysx;
Parasympathetic
Predominace (Nasal
Stuffiness, GI acid
secretion, Diarrhea,
Bradycardia);
Supersensitivity

OTC decongestants; pts
w hypokalemia (b/c
diarrhea causes K loss);

Reserpinede pre ssi on

Reserpine is cheap and effective but as HORRIBBLE SDFX

α blockers (Doxazosin,
end in "-sin")

pts using Doxazosin
were 25% more
likely to have hrt
falu

β Blockers (end in "-ol",
Nadolol, Propranolol,
Timolol, Atenolol,
Bisoprolol, Metoprolol,
Labetalol)

↓ CO via ↓ HR and CF; ↓
CNS; ↓ RAAS (no
compensatory volume
expansion

Bronchospasm (esp
nonselective), Hrt Failr;
Bradycardia; AV block;
Peripheral Vascular Diss
esp in Raynauds:
Depression (not as bad
as Reserpine); Vivd
Dreams; Sex Dysfx

α response → ↑ TPR
and VR;A ten olo l ↑ TPR
(reflex)

NonSelective β blockers
- Asthma, Vascular
Disease

Esp good in white
ppl w hyperkinetic
hearts; Esp good
for Ventricular
Ectopies, Angina,
Sinus Tachycardia
and Dissecting
Aneurysm

↓ TPR, HR, CO, VR
(basically ↓
sympathetics)

Orthostatic Hypotension,
Bradycardia, Heart
block, ↓ CF

Vasodilators
(Hydralazine, Minoxidil,
Diazoxide;
Nirtoprusside))

↓ TPRHyd ra la zin e
Minoxidil Diazoxide:
TPR and VR
Nitroprusside
Hydralazine SLE esp in

slow acetylators ≤
200mg/day, Rapid Drop
in TPR → angina;

Minoxidil Hair growth

↑ K channel efflux → ↓
excitability → ↓ arterial
reactivity/constriction; ↑
blood volume, ↓ in
venous capcitance; ↑
TPR, ↑ HR, ↑ contractility

Nitroprusside (IV
only); Others oral
SDFX = ↓ TPR (all), ↓ HR (V,D>>N), ↓ CF (V>>D,N)
Name
MOA
Pharmacology
Toxicities/SDFX
Reflex
Contraindications
Administration Misc
OK to use w β blockers
Tachycardia
β blockers
All antihypertensive mx cause ↑ in RAAS (via: ↓ BP and CO → ↓ blood flow to kidney → ↑ RAAS), ↑ chance of Orthostatic Hypotension (via ↓ contractilty, volume or CF).
Dyslipidemia Drug Therapy
Name
MOA
Pharmacology
Toxicities/SDFX
Reflex
Contraindications
Administration Misc
Nicotinic Acid/Niacin
Inhibits adipose Lipase
Type I hyperlipidemia
Drug Drug
Interactions
Phenylalkylamine
(Verapamil)

constipation,
Hypotension, some HA,
Peripheral Edema (no
RE to diuretics), AV
block, some CHF

β blockers; Cardiac
Failure
Benzothiazipine
(Diltiazem)

a little hypotension,
peripheral edema, AV
block (nyeh)

considered the
safest Ca channel
blocker
Dihydropyridines
(Nefedipine et al)

Hypotension, HA, Peripheral Edema (does not RE to

diuretics)
w β blockers → ↓ HR
THIS IS BAD!
sublingual, short
duration

highest affintiy x
heart of other Ca
chnl blkrs; good in

ER situation
Drug Drug
Interactions

Reduces esterificationof
TG in liver, May reduce
hepatic cholesterol
formation, Reduces
VLDL, TH and LDL, ↑
HDL, Effective vs
Hyperlipidemia Types II-
V, Cho-ol levels reduced
≈ 25% @ 3gm/day.
clotting via ↑ tissue
plasminogen factor and ↓
plasma fibrinogen

Flushing, Pruitis
(itching), Abdominal
pains, Dyspepsia Peptic
ulcers (at first), Hepatic
dysfx (jaundice, ↑
transaminase levels)

Give w Aspirin; Use
in pts w ↑ ↑ TGs
Poor pt compliance;
Use in pt w ↑ ↑ TGs
Fibrates (Gemfibrozil)
↓ serum TG,

extrahepatic LPL, ↓
aplipoprotein synths, ↑
HDL?

↑ extrahepatic lipoptotein
lipase (LPL), ↓
aplopotrotin syths, ↓
serumTG, ↓ VLDL, kinda
↑ HDL; ↓ plasma
fibrinogen levels ::
Gallstones, ↑ chance of
arrythmias, Nausea,
Cramps, Bleeding due to
↓ platelet adhesiveness
→ bleeding

w Statins = ↑ chance of
Rhabdomyolysis

Use x pts w TH
>750mg/dL, esp
good if pt is Type III
(elevated IDL) phtyp

Indicated x pts w
TG>750 mg/dL; esp
good x Type III
hyperlipidemia;N ot

good x pts w Type I;

Ppl use x ↑ in
surviival w/o
evidence.

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