B: 17-20 Flashcards
Ca2+ ch. blockers
Dihydropiridines: (selectively acts on coronary, arterioles)
-they bind EC portion of Ca ch Alpha-1 subunit
- short acting (T1/2= 6 hrs) : Nifedipine, Nimodipin
- moderate (T1/2= 8-20 hr) : Felodipine, Nitredipin, nisoldipin
long acting (T1/2= 35-50 hr)
Amlodipine,
Manidipin (has duiretic action, inhibit Na, H2o resorption)
Non: (act in heart, coronary, arterioles)
-Bind inner cytoplasmic part of alpha1 subunit
Verapamil, Diltiazem
-NEVER combine with BB bcz cardiac dep, AV block
Dihydropiridines
Nifedipine
Amlodipine
Felodipine
Nimodipine
-they bind EC portion of Ca ch Alpha-1 subunit
vascular >> cardiac effect
Dihydropiridines indications
HTN
Angina
Arrythmias
Prinzmetal’s angina= vasospastic angina
Peripheral vascular disease
-Subarachnoid hemorrhage (Nimodipine)
Hypertensive emergency
Pregnancy HTN (Nifedipine)
Raynaud’s phenomenom
Which drug should wew give in case of Subarachnoid hemorrhage
Nimodipine
Verapamil indications
HTN
Angina (atherosclerotic , vasospastic)
Migrane prophylaxis
Anti arrhythmic class IV: AV node arrhythmia
NO releasing agents
Hydralazine
Hydralazine MOA, adminstration, duration
Induce release of NO from endothelial cells
Mainly arterial vasodil.
Orally active
6-8 h duration
Hydralazine indications
HTN
used in combo with isosorbide dinitrate in heart failure
Induces baroreceptor homeostatic compensatory response; must use w duiretic OR BB
Patient with HF and reduced ejection fraction can be given
Hydralazine + Isosorbide dinitrate
reduce mortality due to heart failure in African Americans.
Hydralazine side effects
Drug induced Lupus at high dose
Tachycardia
Na, H2o retension
causes baro-r homeostatic response ; must be combined with diuretic or BB
Endothelin antagonist
Bosentan
Bosentan indications
Pulmonary HTN
Bosentan side effects
Teratogenic
Hepatotoxicity
PDE-5 inhibitor
Sildenafil
Sildenafil indications
Erectile dysfunction
Pulmonary HTN
Sildenafil side effects
Severe hypotension in combination with Nitrates
Priapism (Prolonges erection)
Blue tinted vision
K sparing diuretics- Aldosteron-R inhibitors
Spironolactone
Eplerenone
steroid inhibitors of cytoplasmic Aldosterone-R in Cortical CD
Spironolactone . eplerenone duration of action
24-72 h
Spironolactone indications
Hyperaldestronism (primary conns disease, + secondary due to chronic HF , or hepatic cirrhosis)
Hypokalemia caused by other diuretics
Antiadronergic
Spironolactone side effects
Hyperkalemic metabolic acidosis (decreases exc of K, H ). (increase exc of Na
Anti-adronergic effect (gynecomastia w/ spironolactone use only)
ACE inhibitors MOA
Inhbition of ACE → ↓ AG-II, ↓ Aldosterone
↑ endogenous vasodilators (Bradykinin)
acts on both arterial and venous ; effectively reduces BP
ACE inhibitors names
Captopril
Enalapril
Perindopril
Ramipril
ACE inhibitors indications
HTN
Diabetic nephropathy
Chronic HF (reduced mortality)
Acute coronary syndrome
ACE inhibitors side effects
Dry cough
Teratogenic
Hyperkalemia
AKI in renal patients
ARB’s
Losartan
Valsartan
Irbesartan
ARB’s indications
HTN
Protective of diabetes nephropathy
CHF (reduced mortality)
like ACE-I
ARB’s side effects
Teratogenic
Hyperkalemia
Drug used in Ischemic heart disease (Angina pectoris)
Nitroglycerine
Isosorbid-mononitrate / dinitrate
CCB
B blockers (Propranonlol)
Ivabradine (inhibit pacemaker If Na channel in SA node)
Trimetazidine (pFOX inhibitor)- inhibit late Na channel in myocardium
Ranolazine (pFOX inhibitor= partial fatty acid oxidation inhibitor ) - inhibit late Na channel in myocardium
Nitrates MOA
Release NO in smooth m
NO stimulates guanylyl cyclase
Increased in cGMP
Dephosphorylation of myosin light chain
Smooth muscle relaxation
Nitrates effects
Vasodilation (venous>>>arterial)
Preload ↓↓
Afterload ↓
Cardiac work ↓
O2 demand ↓
Short acting nitrates
How to give
Onset of action
Duration of acation
Indications
Nitroglycerin
Sublingual
Onset in 1 min
Lasts 10-20 min
Acute angina, pectoris
Acute coronary syndrome
,Hypertensive emergency,
Acute pulmonary edema
Intermediate acting nitrates
How to give
Onset of action
Duration of acation
Indications
Nitroglycerin (also isosorbide mononitrate in oral form)
Oral
Slow onset
2-4 h
Angina prophylaxis
Reduced mortalilty in atients with stable angina
Long acting nitrates
How to give
Onset of action
Duration of acation
Indications
Nitroglycerin
Transdermal patch
Slow
10 h
Angina prophylaxis
Reduced mortalilty in atients with stable angina
Isosorbid-dinitrate
Evrything
Sublingual
short acting
rapidly denitrated in liver, smooth m to isosorbide mononitrate
20-30 min duration of action
Acute angina pectoris
Acute coronary syndrome
Hypertensive emergency,
Acute pulmonary edema
Nitrates side effects
Headache
Reflex tachycardia
Cutaneous flushing
Orthostatic hypotension
Syncope
Methemoglobinemia in prolonged high dosage. (rxn with rbc)
Tolerance after 8-10 h; INTERMITTENT treatment !!
Nitrates contraindications
Systolic BP < 90 mmHg
Right vent. MI (makes it worse because they act on venous side more!!)
Patient took PDE-5 within last 24 h (synergistic relaxation of vascular s.m -> dangerous hypotension, inadequate perfusion to critical organs)
Hypertrophic obstructive cardiomyopathy
CCB used to treat angina
Nifedipine
Verapamil
Diltiazem
B blocker used in angina prophylaxis
Propranolol
L type Ca channel location
- cardiac
- skeletal
- smooth m
- neurons
- endocrine cells
- bone
Blocked by verapamil, DHP
long, large threshold current
T type Ca channel location
heart
neurons
N-type Ca channel location
- neuron
- sperm (also R-type Ca channel
inhibited by Gaba-pentin
pFOX inhibitors
Trimetazidine (pFOX inhibitor)- inhibit late Na channel in myocardium
Ranolazine (pFOX inhibitor= partial fatty acid oxidation inhibitor ) - inhibit late Na channel in myocardium
increase efficiency of O2 utilization by shifting heart preferance from fatty acid to glucose.
SE: QT prolongation
