Nitrates Flashcards
Drugs that relieve anginal pain by dilating veins and coronary arteries.
- They act directly on smooth muscles to cause relaxation in both arteries and veins of blood vessel walls which results in vasodilation and relieving anginal pain.
- O15-60min, D0.-12hrs
- Metabolized in the Liver, excreted by the kidneys
- Action directly on the muscles, these doesnt influence nerves
Nitrates
The vasodilating effect of the nitrate (No2) group results from the fact that nitrate is converted to ______
Nitric oxide (NO)
Dilation of ____ decreases blood return to the heart, so the heart vessels contain only a small volume of blood. Therefore less volume of blood to pump.
Veins
Nitrates dilate ____ at high doses, resulting in increase blood flow to ischemic areas of the heart.
coronary arteries
Nitrates dilate arterioles, thus causing lower ___ which causes low systolic BP (lower afterload of the heart)
PVR
Biochemical steps on Nitrates
Nitrate - Vascular Smooth muscle - Interact with muscle chemical to form Nitric Oxide (active form) - activates enzyme that catalyzes GTP - GTP converted to c-GMP - decrease intacellular Ca++ levels - VASODILATION
2 types of organic nitrate
short acting and long acting
organic nitrate that is taken sublingually and quickly stops acute angina attack in progress
short acting organic nitrate
organic nitrate that is taken orally or via transdermal route decrease the frequency and severity of angina episodes. It also decreases the symptoms of HF.
Long acting organic nitrate (isosorbide dinitrate)
For ____, Nitrates causes dilation of the vein and arteries, leading to reduced mycardial o2 demand and more efficient distribution of blood in the myocardium
MI
For _____, nitrates causes reduced peripheral resistance hence peripheral vasodilation and lowering of BP.
HTN
______ is used to manage angina that is unresponsive to nitrate via other routes or to beta blockers. IT is also used to reduce pre-and after-load in sever HF.
IV nitroglycerine
Nitrate Agents (4)
- Nitro-glycerine (NTG)
- Isosorbide dinitrate
- Isosorbide mononitrate
- Amyl nitrate
Nitrate agent that is sublingual, 1 tab or spray every 3-5 mins; max dose is 3 in 15 mins) most important drug for angina.
- Oral forms rapidly metabolized by the liver and only small proportion reached systemic circulation, hence spray form and IV more effective.
- sublingual form absorbed directly into blood, acts within 1-3 min and lasts 30-60 mins.
- ointment effective for 4-8 hr but onset is slow
- transdermal form effective for 12 hr but onset is slow
- can be carried by pt who then can use it prn
- slow-release forms are available for use prevent angina attacks
- adverse effects include hypotension, headache, dizziness, tachycardia, rash, flush, sweating, and chest pain
Nitro-glycerine (NTG) spray = Nitrostat ER buccal tabs = Nitogard SR lingual aerosols = nitrolingual ER caps = Nitrocap parenteral inj. = Nitrobin/Nitrol ointment = Nitro Bid and Nitrostat Transdermal topical sys = Nitro-disc, Transderm-Nitro and Nitro-dur
Nitrate agent that is sublingual and acts about 2 min and effective for 2-3 hr
- used to reduce freq. and severity of acute anginal episodes
- high oral dose produces effect in 30 min and last for 4 hrs.
- sustained release has onset of 4 hrs
Isosorbide dinitrate
Nitrate agent that is a metabolite and active component of isosobide nitrate
- available in regular and er tabs for once a day use 30-60 mg
Isosorbid Mononitrate
Nitrate agent that is a volatile liquid that is packaged in crushable glass caps surrounded with cotton and gauze. When capsule is crushed, the liquid vaporizes and is directly inhaled by the pt.
- onset 30 sec upon inhalation
- Used as antidote for cyanide poisoning and cardiac function tests
- abuse is common and dangerous
Amyl Nitrate
Contraindication for Nitrates
Hypersensitivity.
Sever anemia
Hypotension, Hypovolemia
Pts with cerebral hemorrhage or other head injury bc it elevates CSF (intracranial pressure)
Cardiac tamponade or constrictive pericarditis
Hypothyroidism
Nitrates shouldnt be taken with _______ (ie. Viagra or vardenafil, tadenafil, ED drugs) bc it cause hypotension. (shouldnt be taken within 24 hr)
phosphidieterase enzyme type 5
Assessment on Nitrates
Assess for chest pain on scale 1-10 before administration of nitrate and 5 mins after.
For long acting, monitor for OH- take BP on both arms sitting and standing.
For ointment measure BP, pulse, etc. 10 min after administration
Repeat vitals measure 1 hr after administration
Remove patch after 6-12 hrs or withhold oral organic nitrate to reduce tolerance
Pt teaching for Nitrates
Avoid alcohol, stressful situations that cause angina, take med 5 min before stressful event
always carry nitrate,
anticipate light-headedness and slight headache
report dry mouth, blurred vision, severe headache (signs of overdose)
dont apply ointment using fingers
ER tabs/caps not to be used at bedtime (may cause aspiration)
take oral/sustained release on empty stomach (1hr before meal or 2 hrs after meals)
Occurs when an area of the heart dies due to insufficient o2 due to CAD, thrombus formation in coronary artery, heavy exertion and abrupt increase in BP.
- Drugs used to treat this are (9)
Acute MI
- Thrombolytics
- ASA
- Morphine Sulphate
- ADP receptor blockers
- Beta blocker
- Ca+ channel blocker
- ACE Inhibitors
- Platelet glycoprotein IIb and IIIa
- Narcotics
On diagnosis of MI, pts are usually placed on ____ to prevent new thrombus formation, later they may be placed with _____ or ______. These are used to limit the damage to the myocardium and prevent cardiogenic shock by increasing o2 rich blood to myocardium.
Heparin
Warfarin, LMWH
First drug to be administered in MI, prevents clotting and coronary artery constriction. Used in weeks following acute MO, it reduces mortality (160-325mg/day) Low dose (75-15mg/day) used as maintenance therapy.
ASA
New agents approved for prevention of thrombotic stroke and MI. Given to pts allergic to ASA or at risk of bleeding from ASA.
Adenosine di-phosphate (ADP) receptor blockers
Drug that reduces myocardial o2 demand, given with Nitro-glycerine
Morphine Sulphate
Drugs that reduces hearts o2 demand by decreasing HR. They also cause slow impulses within the heart thus decrease risk of dysrythmias. Helps to decrease MI mortality.
Beta-blocker (atenolol, lopressor)
Drugs used to inhibit platelet aggregation. Used for unstable angina or MI.
Platelet glycoprotein IIb and IIIa. (abciximab-ReoPro)
Drugs administered after acute MI. They reduce risk of CHF and death.
ACE Inhibitors
Drugs used by interfering with Ca++ transport; they decrease myocardial o2 and increase o2 supply demand.
Calcium blockers
For pain management in acute MI, ____ are used. (ie. ____and ____)
Narcotics. Morphine sulphate or meperidine
Variety of diseases associated with blood vessels outside the heart, but it generally refer to disease of BV of the arms and legs. (the exremeties)
PVD
Two types of PVD
arterial and venous origin
Tx of PVD (3) that cause increased peripheral blood flow
Hemorheologic agents, Vasodilators, antiplatelets
A condition that causes some areas of your body — such as your fingers, toes, the tip of your nose and your ears — to feel numb and cool in response to cold temperatures or stress. In this disease, smaller arteries that supply blood to your skin narrow, limiting blood circulation to affected areas.
Raynaud’s disease (arterial vasospasm)
Drugs used to treat Raynauds disease (4)
- Calcium Ion Antagonists
- Adrenergic Antagonists
- ACE Inhibitors
- Direct Vasodilators
A rare disease of the arteries and veins in the arms and legs. In this disease, your blood vessels become inflamed, swell and can become blocked with blood clots (thrombi). This eventually damages or destroys skin tissues and may lead to infection and gangrene.
Buerger’s disease (thromboangiitis obliterans)
Drugs used for Tx of intermittent claudication by decreasing blood viscosity and improve its flow properties. It also increases RBC flexibility, decrease concentration of fibrinogen in blood, and prevent aggregation of platelets and RBC.
- It causes improved tissue perfusion with reduce freq. of pain, improved tolerance to exercise, and imporved peripheral vascular pulse.
Hemorrheologic Agents (ie PENTOXIFYLLINE)
3 Types of Vasodilators used in Tx of PVD
- Alpha-adrenergic antagonist
- Beta-adrenergic stimulant
- Papaverine
Vasodilator used to treat PVD that dilates cerebral and coronary blood vessels and inhibits atrial and ventricular premature contraction and ventricular dysryhtmia
Pepaverine
Drugs used in Tx of PVD.
- Suppress cAMP phophodiesterase II causing increased levels of cAMP = vasodilation and inhibits of platelet aggregation.
Platelet Aggregatior Inhibitor (CILOSTAZOL)
Contraindication with PVD drugs
Pts with pace makers
a condition that causes damage to your eye’s optic nerve and gets worse over time.
Glaucoma
In Tx of PVD, monitor pts
Skin condition and Glaucoma
Abnormal condition in which cardiac pumping is impaired as the result of myocardial infarction, ichemic heart disease, or cardiomyopathy.
Heart Failure
Failure of the ventricle to eject blood efficiently results in _____, causing chamber dilation, and elevated intra-cardiac pressure.
Volume overload
The backward trasmission of hydrostatic pressure from the left ventricle leads to ______.
pulmonary congestion
Elevated right ventricular pressure leads to _______ and ______.
systemic venous congestion and peripheral edema
Drugs Tx for HF
Combination of vasodilators (IV nitro-glycerine, nitroprusside, nesertide) inotropic and diuretic therapy. ACE Inhibitors are the mainstays of oral vasodilator therapy.
Rythms generated by SA node
Sinus rythms
Rythms generated by AV node
Nodal rythms
Vagal fibers located near SA node, Atria, and ventricles slow down HR by inhibiting _____ and ____ of the heart.
Impulse formation and electrical conduction
____ released by the SNS increases HR by promoting impulse formation and electrical conduction of the heart.
NE
First-line therapy for acute HF (symptomatic pts)
ACE Inhibitor + beta-adrenergic blocker (BB)
or
Angiotensin II receptor blocker (ARB)
As Tx and HF progresses.. drugs? (4)
ARB, Digoxin, Nitrates, Diuretic and Aldosterone Inhibitor
Drug used in pts with HF. Its used for its positive inotropic effect. Cannot give to pts with allergy, atrial or ventriculat fib, and tachycardia.
Digoxin
short term Tx of HF with pts who havent responded adequately to Digoxin and vasodilation therapy. It blocks SNS stimulation of beta receptors in heart and decrease risk of ventricular fib.
- Monitor HR, rythm, arterial BPl arterial gas ex., urine output.
Inotropic Vasodilators (Phosphodiesterase Inhibitors) - Milrinone (Primacor) IV use not established for children
Drugs used in Tx of ventricular tachycardia and fib., conversion of AF to AF normal sinus rythm, maintainance of sinus rythm.
- It prolong duration of the AP, slow repolarization, and prolong the refractory period in the atria and ventricles.
Class II K+ Channel Blockers
Drugs used in Tx of supra-ventricular tachycardia (SVT) by blocking the movement of Ca++ conductile and contractile myocardial cells resulting in firing of SA and AV nodes, slow conduction and prolong the refractory period in the AV node.
Class IV Ca++ Channel Blockers
- dilitazem (Cardizem), verapamil (Calan, Isoptin), adenosine, magnesium sulphate.
Dysrythmias are common in elderly pts but only those causing symptoms of ______ are treated with dysrhythmitic drugs.
circulatory impairment
Chest discomfort arising from the heart bc of lack of o2 in the heart cells. Symptoms of CAD aka IHD.
Angina pectoris
Develops when the o2 supply needed by heart cells is inadequate due to atherosclerosis or arterial spasms.
CAD or IHD
3 types of angina.
- Classical Angina
- Variant Angina
- Unstable Angina
Type of Angina that is due to narrowing of the coronary vessels resulting from fat deposit (atheroma) on the walls of the arteries
Classical Angina
Type of Angina wherein the arteries are narrowed by contraction (spasm) muscle fibres in arterial walls, and pain in chest may occur.
Variant Angina
Drug agents in Tx for unstable angina.
platelet-active agents
Drugs in Tx of elevated LDL cholesterol
HMG-CoA reductase inhibitors (statinss)
Class of Angina.
- ordinary physical activity doesnt cause angina but with strenous, rapid or prolonged exertion at work or recreation.
Class 1
Class of Angina.
- slight limitation of ordinary activity angina occurs on walking, climbing stairs rapidly, walking uphill, walking or stair climbing after meal, or in cold, in wind or under emotional stress. Walking more than 2 blocks on the level and climbing more than one flight of ordinary strairs at a normal pace and in normal conditions can elicit angin.a
Class 2
Class of Angina.
- MArked limitations of ordinary physical activity. Occurs on walking one or two blocks on a level and climbing one flight of stairs in normal condition at a normal pace.
Class 3
Class of Angina.
- Ibability to carry on any physical activity without discomfort-anginal symptoms may be present at rest.
Class 4
Tx for pts with occasional angina attacks
Rapid-acting nitrate (Nitroglycerin)
Tx for pts with more frequent anginal attacks
Preventative tx including beta blockers, long-lasting nitrate, Ca++ blockers
6 groups of drugs used for Tx of angina pectoris
- Nitrates
- ACE Inhibitors
- Ca++ channel blockers
- B-Adrenergic blocking agents
- Statins
- Platelet-active agents/Anticoagulants such as ASA, Heparin/LMWH
Drugs used for Tx of Angina
- Vasodilator for mild CHF
- reduce after load by blocking angiotensin II mediated peripheral vasoconstriction and help reduce circulating blood vol by inhibiting secretion of aldosterone.
- reduce BP, relax smooth muscles and cause pooling of the blood in the veins, preserve CO, and increase renal blood flow
- Effect is improved CO resulting in improved tissue perfusion
ACE Inhibitors
Drugs used for Tx of Angina
- decreased blood volume leading to decreased venous return and decreased BP,
- decrease preload and afterload
Diuretic (Lasix)
Drugs used for Tx of Angina
- exhibit negative inotropic effect
- Tx CHF due to high SNS activity
- Inhibits SNS activity - reducing HR and BP. Workload on the heart is reduced after some months, and the heart size, shape and function returns to normal.
Beta-adrenergic blockers
Drugs used for Tx of Angina
- organic nitrate
- reduces venous return leading to decreased cardiac workload, thus decreased pulmonary congestion and peripheral edema
- dilates coronary arteries allowing greater inflow of oxygen to the cardiac muscle
Direct Vasodilator
- Isosorbide Dinitrate (Isordil)
Drugs used for Tx of Angina
- Hormone normally secreted by the heart in response to fluid and pressure overload
- Vasodilator in clients with severe heart failure
- helps heart ot recover deteriorating function by decrease preload and postload pressure, increase diuresis and sodium excretion, suppressing the RAAS and reducing NE secretion
- reduce heart workload and improve symptoms
Natriuretic PEptides NESIRITIDE
Abnormal heart rhythm associated with impaire conduction system. Occurs when there is a disturbance of the normal electrical conduction resulting in an abnormal heart muscle contraction or heart beat. Can originate in any part of conduction system or atrial or ventricular muscle.
- Caused by firing of abnormal pacemaker cells, or the blockage of normal electrical pathways or a combination of both.
Dysrhythmia (Arrhthymia)
Drug used for brady-dysrhythmia
Atropine
Drug used for AF. Convert to normal sinus rhythym.
Digoxin
Drugs (class) Tx for symptomatic premature ventricular contractions, supra tachycardia and ventricular tachycardia, prevent ventricular fibrillation.
- they block movement of Na+ into cells of the cardiac conducting system resulting in decreased formation and conduction of electrical impulses
Class 1 Sodium Channel Blockers
- Class 1A (Quinidine P) Procainamide (Procan PR) Disopyramine (Rhytmodan) - supra tachycardia
- Class 1B (Locaine P) Mexiletine (Novo-Mexiletine) Phenytoin (Dilantin)
- CLass 1C (Flecainide) Propafenone
Agents for Dysrhythmia (2)
Class 1 Sodium Blockers
Class II Beta Blockers
DRUGS THAT REDUCES LIPID LEVELS
Antilipemics
Protein component of lipoprotein
Apo lipoprotein
Most lipids entering the blood bind to blood plasma protein _____
Albumin
Conjugated proteins in which lipids from an integral part of the molecule. They are synthesized in the liver, contain various amts of triglyceride, cholesterol, phopholipids, and protein. Classified according to type of apo___ they contain and density.
Lipoprotein
The greater the proportion of lipid in the lipoprotein, the ____ the lipoprotein density
lower
Minute droplets of lipoproteins
-the form in which dietary fats are absorbed from SI. Consist of 90% triglycerides and small amts of cholesterol, phospholipids and protein.
Chylomicrons
Normal cholesterol values
240 mg/dl
Normal triglyceride values
160 mg/dl of blood
Primary Tx of hyperlipidemia
Weight reduction, exercise and diet low in cholesterol and fat.
After starting lipid drug therapy, LDL-C level should be measure at __to___ weeks and again at __mos.
4-6 weeks
3 months
4 kinds of lipoprotein disorders
- Familial HC
- Polygenic HC
- Familial HT
- Mixed hyperlipidemia
C means
Cholesterol
HC means
Hypercholesterolemia
HT means
Hyper-triglyceridemia
HMG-CoA (Statin) means
hydroxymethylglutaryl coenzyme A
Lipoprotein disorder characterized by ↑ LDL-C. Drug therapy statin, bile acid resin, and niacin.
- comb theraphy = bile acid resin + niacin statin + bile acid resin, niacin + statin.
Familial HC and Polygenic HC
Lipoprotein disorder characterized by ↑Triglyceride.
- drug therapy include fibrate + niacin.
Familial HT
Lipoprotein disorder characterized by ↑LDL-C and Triglyceride.
- drug therapy include niacin, statin, fibrate.
- comb therapy Niacin + statin, niacin + bile acid resin, niacin + fibrate
Mixed hyperlipidemia
4 Drug Agents for Hyperlipidemia
- Bile Acid- Binding Resin
- HMG-CoA REductase Inhibitor (Statins)
- Niacin (Nicotonic Acid)
- Fibric Acid
Large resin, not absorbed by the SI that binds bile acid and cholesterol keeping them in lumen. Hence they are not absorbed systematically. Removal of cholesterol cause liver to make more LDL receptors and so remove more cholesterol to the serum.
- Bc of the removal of the bile acids, liver cells increase metabolism of cholesterol to produce bile acids thus reducing LDL and total cholesterol levels.
- Side effects include rash, bloating, constipation, decrease abs of vitK, A and D, muscle ache and pain.
- Take before (1hr) meal or after meal (4hrs)
- Follow bulk diet and drink lots of fluids
- Supplements may be necessarty
- REport skin and eye changes
Bile Acid-Binding Resin
Cholesterol is made by the lover by using _____.
acetyl Co A
Drug agent for Tx of Hyperlipidemia
- Decrease synthesis of cholesterol by inhibiting a certain enzyme. Result in the liver developing more LDL receptor and so remove LDL from the blood. End result is lower LDL and cholesterol in blood, which slows CAD and reduces CVD mortality.
- adverse effect include GI, flatulence, cramps, abdominal pain, and constipation. Rhabdomyolysis
HMG-CoA Reductace Inhibitor (Statins)
Enzyme that serves as a major site of cholesterol synthesis.
HMG-CoA reductase.
Drug agent for Tx of Hyperlipidemia
- 2-3g/day - 25mg/day as a vit treatment
- Inhibits VLDL synthesis in the liver, which cause decrease in LDL and triglyceride production.
- effect is decreased LDL and triglyceride and increase of HDL levels.
- adverse effect more than statins, hot flashes, flushing and nausea, gas, diarrhea
- no megadoses, take with COLD water, with or after meal
- report abdominal, joint or stomach pain, skin colour changes, yellowing of sclera
Niacin (Nicotinic Acid)
Drug agent for Tx of Hyperlipidemia
- lower lipid levels and VLDL, largely replaced by statins, but used in combination with them.
- Tx for hypertriglyceridemia
- keep all medical follows and lab app
- report brusing, bleeding, muscle cramps, stool colour
Fibric Acid
- fenofibrate, gemofibrozil
