Cardiovascular System Flashcards
Renin is secreted by
JG cells of macula densa of affereent arteriole
Organs that angiotensin 2 acts (6)
Heart: increase force,rate,velocity
Bv: vasoconstriction
Kidney : sodium,water retention
Adrenal : aldosterone secretion
Brain: increase ADH, increasing thirst receptors —> plasma expansion
Peripheral nerves: activation of sympathetic system
ACEI …….TPR
Preload ,after load
Decreases
Decreases
All are carboxyl groups except
Captopril -sulfhydryl
Fosinopril: phosphinate
All are prodrug except …
Captopril
Lisinopril
Max and min bioavailability of ACEI
Max :70%: captopril
Min : 25%: lisinopril
All are excreted by kidney except
Fosinopril: liver:kidney = 50/50
Uses of ACEI and ARB
Home Care Makes Patient Definitely Strong
HTN
CHF
MI
PX of MI
DN
Scleroderma crisis
Use of aliskiren
Only HTN
Adverse effects of captopril
CAPTOPRIL
Cough
Angioneurotic Edema
Potassium high
Tetatogenic, taste prob
Other: fatigue,headache
Proteinuria-rare
Renal impairment
Itch
Low Bp -first dose hypotension- give 1/2 dose for 1st week then from 2nd week onwards full dose
C/I of captopril
Pregnancy
Allergy
Renal artery stenosis : u/l or b/l
Hyperkalemia
Antihypertensive that is also antidiabetic
Telmisartan - has PPAR gamma activating property
Known as cardio metabolic Sartan
Losartan in anticoagulation
Blocks thromboxane A2 , inhibit plt aggregation
( losartan activity is similar to aspirin, hence it’s also a uricosuric drug)
Adverse effects of aliskiren (4)
Angioneurotic edema
Hyperkalemia
Teratogenic
Hypotension
MOA of digoxin w.r.to HR
Decrease HR without decreasing myocardial oxygen consumption
Name 4 cardiac glycosides
Digoxin
Digitoxin
Ouabain
Strophanthin
Where are digitalis obtained from
Digoxin: Digitalis Lanata
Digitoxin: Digitalis purpura
Actions of digitalis (4)
- Heart:
Increase force of contraction
Increase excitability
Decrease velocity —> decrease HR - Blood vessels: vasodilation
- Kidney: diuresis
- CNS: activate CTZ —> N/V
Elimination of digitoxin vs digoxin
Oral availability
Digitoxin: hepatic
Digoxin: renal
Digitoxin: 90-100%
Digoxin: 60-80%
Plasma protein binding for digitoxin vs digoxin
Toxicity of digitoxin vs digoxin
Digitoxin: 95%
Digoxin: 25%
Digitoxin: >35ng/ml
Digoxin: >2ng/ml
Toxicity of digitalis
Hypokalemia
Hypercalcemia
Adverse effects of digitalis (3)
N/V
Yellow vision
Gynecomastia
ECG finding of digitalis (4)
Increase PR
Decrease QT
T wave inversion
ST depression
Antidote of digitalis
Anti-dig Fab fragments
Nitrates MOA (2)
Increase in CGMP which
1. Inhibit calcium channel
2. Inhibit MLCK phosphorylation
Uses of nitrates (6)
A: Angina pectoris
B: biliary colic
C : cyanide poisoning
D: dil ka daura: MI
E: esophageal spasm
F: failure : HF
How does nitrates work for cyanide poisoning?
- Hb—-> methb ( sodium nitrite)
- Methb——-> cyanohb ( cyanide)
- Cyanohb——-> methb + sodium thiocyanate (sodium thiosulfate)
Sodium thiocyanate gets excretes in urine
Adverse effects of nitrates
T: tolerance
D: dependence
S: skin rashes
R: reflex tachycardia
O: orthostatic hypotension
M: methb
C/I of nitrates (3)
- Right ventricular infarction
- Sildenafil
- HOCM
All nitrates undergo first pass metabolism except
Shortest acting nitrate:
Longest acting nitrate :
Isosorbide mononitrate
Shortest: GTN / Amyl nitrite
Longest: Pentaerythitol
MOA of nicorandil (2)
- K channel opener : hyperpolarizes smooth muscle membrane and relaxes it.
- Acts as nitric oxide donor- relaxes blood vessels by increasing cGMP
How does nicorandil exert cardio protective action?
Stimulates ischemic preconditioning —as a result of mitochondrial K ATP channels
Uses of nicorandil (2)
- 2nd line antianginal drug
- Resistant asthma
MOA of ivabradine
Blocks HCN channel responsible for pacemaker funny current - which regulates heart rate.
Another name for ivabradrine
Pure heart rate blocker
As it only blocks funny currents.
Uses of ivabradine (3)
- Stable angina
- Sinus tachycardia
- Stable with symptomatic chronic HF with resting HR >70bpm
Those on max tolerated beta blockers
Have c/I to beta blockers
Moa of ranolazine
Inhibit late inward sodium current.
Reduces diastolic wall tension and oxygen consumption
Not affect HR contractility.
Uses of ranolazine
Angina refractory to other therapies
Adverse effects of ranolazine (5)
Constipation
Dizziness
Headache
Nausea
Qt prolongation
MOA of trimetazidine. Use
Inhibits mitochondrial LC3KAT, responsible for fatty acid oxidation
Use: add on therapy in angina and post Mi
Different between dihydropyridines and non dihydropyridines
Dihydro: act on smooth muscle
More potent, lipophilic
Non dihydro: act on heart
Negative chrono,iono,dromo
MOA of CCB
Block voltage dependent calcium L type channels.
Use of nimodipine
Subarachnoid hemorrhage- prevent cerebral vasospam
Uses of non DHP (2)
Antiarrythmic - atrial flutter,atrial fib
HTN
Other than CCB action, action of
1. Nifedipine
2. Verapamil
- Tocolytic
- HOCM
Adverse effects of CCB
Specific effects of DHP and non dhp
Gum hyperplasia
Dhp: flushing,
peripheral edema,
dizziness
Non dhp:
Av block
Constipation
Hyper prolactinemia
CHF due to cardiac depression-verapamil
C/I of digitalis
C/I: carditis-myocarditis
In: increased calcium
Weak : WPW syndrome
H: hypokalemia,hypomagnesemia
E: elderly
A: AV block
R: renal failure
T: thyroid: hypo/hyper.
High ceiling diuretics (2)
Furosemide
Bumetanide
Name the ionotropic drugs classification
- Cardiac glycosides:
Digoxin, Ouabain - Sympathomimetics:
dopamine, dobutamine - PDE 3 inhibitor:
Amrinone, Milrinone
MOA of hydralazine
Directly acting vasodilator: Increases cGMP, reduce TPR , reduce after load
Uses of hydralazine (3)
- HTN emergency
- HTN in pregnancy
- Coadministered with beta blockers to prevent reflex tachycardia
Main S/E of hydralazine
Others (2)
Drug induced SLE
- Reflex tachycardia ( flushing, throbbing headache)
- Fluid retention
Rapidly acting vasodilator with brief duration of action (2-5 mins) when given iv
Sodium nitroprusside.
MOA of sodium nitro Prusside
Endothelial cells and RBC split nitroprusside to relax vascular smooth muscle through cGMP.
Main problem with sodium nitroprusside
Can release cyanide- cyanide toxicity
Bp and Hr with clonidine
Fall in bp
Fall in HR( bradycardia )
Adverse effects of clonidine (6)
- Sedation
- Mental depression
- Sleep disturbance
- Dryness of mouth,nose,eyes
- Postural hypotension
- Withdrawal syndrome
Other uses of clonidine besides rx HTN (4)
- Opioid withdrawal
- Analgesic
- Menopausal syndrome- to attenuate vasomotor symptoms
- Control loose motions in diabetic neuropathy
Alpha methyldopa is converted to ….
MethylNA - selective alpha 2 agonist
S/e of methyl dopa
Coomb’s positive haemolytic anemia
Methyldopa is DOC for …..
HTN in pregnancy
S/e of spironolactone (3)
Gynecomastia
Erectile dysfunction
Menstrual prob
Anti HtN with sexual side effects (4)
- Thiazides
- Beta blockers
- Clonidine
- Prazosin
Drugs with SLE symptoms
SHIP
Sulfalazine
Hydralazine
INH
Procainamide
They are slow acetylators
MOA of diazoside
K+ channel opener
Arterial dilation-decrease bp
On pancreas: decrease insulin release-DM
Diuretics that cause hyperlipidemia (3)
Thiazides
Furosemide
Beta blockers
AntiHtN good for dyslipidemia
Alpha blockers : decrease LDL,TG
Chronic HTN, Ortho static hypotension is maximum with …..
Guanethidine
Anti htn drug that can’t cause bradycardia
Hydralazine- reflex tachycardia
* all drugs that block sympathetic nervous system have bradycardia.
HTN emergency is defined as ….
> 180/120 with end organ damage
Htn with end organ damage DOC is …(3)
- Nicardipine
- Labetalol
- Claridipine
Drug indicated for PIH
Mild-moderate: labetalol (oral) >methyldopa>DHP
HTN crisis: iv labetalol > hydralazine
Antihtn to be avoided in pregnancy (4)
- ACEI/ARB
- Diuretics- placental hypoperfusion
- Nitroprusside: cyanide
- Atenolol: LBW
Drugs that decrease plasma renin (2)
- Beta 1 blockers
Clonidine - NSAIDS
Drugs that decrease plasma renin activity
Aliskiren
Eg of ARNI
Use
Sacubitril
ARB + Neprilysin inhibitor
Use: CHF
MOA of action of sacubitril
BNP ———-> broken down ( neprilysin)
( neutral endopeptidase)
Neprilysin also breaks bradykinin, AT1
Drug interaction of sacubitril
If given along with ACEI; excessive increase in bradykinin —> severe angioedema
Losartan is a ……drug
HTN with DM and b/L renal artery stenosis , DOC…
Uricosuric
Amlodipine
Drugs which prolong qt interval
Class 1a, class 3
Class 1a:
Queen: quinidine
Protects: procainamide
Discopyramide: disopyramide
Class 3:
A: amiodarone
I: ibutilide
D: dofetilide
S: Sotalol
S/e of quinidine (5)
- Increase QT interval —> TdP
- Salicylism
- Cinnchonism
- Release of insulin—> hypoglycaemia
- Anticholinergic action : causes A. Fib
—> paradoxical tachycardia
S/E of lignocaine
Non cardiotoxic but neurotoxic
Early signs:
Nystagmus, Ataxia
Paresthesias
Late signs: Seizures
Coma
Drugs that cause AV block
ABCD
A: Adenosine
B: beta blockers
C: CCB
D: Digoxin
Lithium
Antiarrhythmic class 1a, class 3
MOA of adenosine
Hyperpolarization of AV node —> AV conduction decrease
Adenosine acts on adenosine A1 receptors and cause bronchoconstriction of lungs , thus theophylline, which is adenosine antagonist is given.
Medical defibrillator is ….
Bretylium
All antiarrythmics are category C except ….
Amiodarone- category D - also phenytoin,atenolol
S/e of adenosine
S/e of sotalol
Cough, flushing
Bronchospasm-beta blocker effect
MOA of ezetimibe
In the presence of statins, cholesterol level in the liver decreases, liver gets GIT to increase cholesterol absorption via NPC1L1.
Ezetimibe is NPC1L1 inhibitor.
S/E of statins
Increased risk of myalgia when given along with
1. CYP3A4 inhibitors
Azoles,macrolides,warfarin,amiodarone,ritonavir
- Niacin
- Gemfibrozil
Moa of gemfibrozil
PPAR alpha agonist
Increase LPL—> hydrolysis of TG
( break down VLDL, CM)
Decrease TG levels
Mc s/e of fibrates is ….
C/I in …..
Gall stones
Renal failure
MOA of bile acid resins
Bind to bile acid in the intestine and excrete it in stool, thus preventing enterohepatic circulation.
Decrease liver synthesis of cholesterol will cause increase in LDL-R, which decreases plasma LDL.
S/e of bile acid resins (5)
- Bad taste
- Low efficacy
- Interfere with absorption of ADEK
- Increase TG
- Gi sm:
constipation, dyspepsia,flatulence
MOA of nicotinic acid
Inhibit lipolysis (hormone sensitive lipase) in adipose tissue
S/e of niacin
Flushing - to be given with aspirin to decrease flushing
Hyperuricemia
Hyperglycaemia
Drug which
1. Max decrease LDL
2. Max decrease TG
3. Max increase HDL
- PCSK9 > statins
- Fibrate
- Niacin
Antihypolipidemic safe in pregnancy
Resin»>Fish oil
MOA of lomitapide
Microsomal TG transfer protein inhibitor
Decrease VLDL production
S/e of lomitapide
Use
N/V
Increase hepatic fat
Homozygous familial hypercholesterolemia
ApoB inhibitor is …..
S/e
Use
Mipomersen
Injection site reaction
Flu-like symptoms
Homozygous familial hypercholesterolemia
Moa of PCSK9 inhibitor
Pcsk 9 from blood binds to LDLr and cause degradation.
PCSK9 inhibitor inhibits that.
Eg: Alirocumab,Evolucumab
S/e of PCSK9 inhibitor
Use of PCSK9 inhibitor
Myalgia
Dementia
Delirium
Use : heterozygous familial hyper cholesterolemia
Drug inhibiting PCSK9 synthesis
Inclisiran
Most potent statin
Statin with highest bioavailability
Rosuvastatin
Pitavastatin
When should statins be taken?
Rosuvastatin -19hrs
Atorvastatin-17hrs
Pitavastatin- 12 hrs
Can be taken at any time during the day
All others at bedtime, as HMGCOA reductase activity is max at night.
Statins are usually given for children > 10 years except …..
Pravastatin -> 8 years
Prophylaxis of hyperlipidemias (2)
- Gugulipid
- Fish oil (omega 3 FA)