Term
A 59 year old male with a history of HTN, T2DM, and Dyslipidemia presents to the Emergency Room with a 4 hour presentation of substernal, stabbing chest pain, shortness of breath and diaphoresis. Your ER crew is starting oxygen and placing EKG leads.
Which of the following medications would be the most appropriate to give at this point: |
|
Definition
|
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Term
|
Definition
- Streptokinase
- rTPA
- Reteplase |
|
|
Term
| Indications for Thrombolytic Drugs: |
|
Definition
- Acute MI
- Pulmonary Embolus
- Deep Vein Thrombosis
- Iscemic stroke (CT or MRI first) |
|
|
Term
| Recombinant Tissue Plasminogen Activator is in the form of __, __, and __. These are produced by genetic engineering and have half life of 3 min. These are ___. The serious adverse effect is ___. |
|
Definition
- rTPA, Alteplase, and Activase
- expensive
- hemorrhage |
|
|
Term
| CI to Thrombolytic drugs: |
|
Definition
- previous surgery in the past few weeks
- trauma
- previous stroke and now giving it for heart
- bleeding problems |
|
|
Term
| Reteplase is a __ genetically engineered form of r-TPA. It diffuses more freely into the clot than Alteplase and has a ___ half life than Alteplase. |
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Definition
|
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Term
| Streptokinase is a ___ ___ of ___ extracted from hemolytic streptococci. A __ __ has to be used to saturate preexisting antibodies. __ __ is a potential side effect. |
|
Definition
- nonenzymatic activator of plasminogen
- loading dose
- Serious hemorrhage |
|
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Term
|
Definition
- Aspirin
- Clopidogrel, Ticlodipine
- Dipyridamole
- Cilostazol
- Pentoxifylline
- Abciximab, Eptifibatide, Tirofiban
(ACDC PA) |
|
|
Term
| Aspirin is good for pple who are having Mis to prevent further platelet aggregation. Aspirin blocks cyclooxygenase ____. Inactivates for 7 days. Dose: 1 81mg tablet. Normally 325mg for pain. Don’t give that much b/c GI bleed. |
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Definition
|
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Term
| Aspirin at very low doses ___ inhibits __ in platelets. Since platelets cannot synthesize new enzyme, aspirin inhibits ___ formation and platelet aggregation for the life of the platelet (7-10 days). In contrast, endothelial cells can synthesize new cyclooxygenase. |
|
Definition
- irreversibly
- cyclooxygenase |
|
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Term
| Aspirin therapeutic uses: |
|
Definition
- Primary prevention of Cardiovascular disease
- Secondary prevention of MI and stroke
- All patients with MI
- Artificial heart valves, hemodialysis, and CABG pts should get ASA to reduce thromboembolic complications |
|
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Term
| Don't give ASA to pts with ___ ___. |
|
Definition
|
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Term
| Clopidogrel has a __ onset (_hrs). Often used in combo with __ in high risk situations like with __ and __ __ __. This can also be used with __. |
|
Definition
- slow (2hr)
- ASA
- stents
- Acute Coronary Syndrome
- MI |
|
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Term
| Clopidogrel is indicated for prevention of __ __ in ___. Has better outcomes than ASA but is very ___. |
|
Definition
- ischemic events in atherosclerosis
- expensive |
|
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Term
| Abciximab (ReoPro) is a __ __ that prevents __ binding to __ __ __ and __, thus inhibiting __ __. It has greater antithrombotic activity than __ or __. It is approved as antithrombotic during ___. |
|
Definition
- monoclonal antibody
- fibrinogen
- Glycoprotein GP IIb and IIIa
- platelet aggregation
- than ASA or heparin
- angioplasty |
|
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Term
| Approved antithrombotic drug during angioplasty: |
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Definition
|
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Term
| Other monoclonal antibodies include __ and __, which are approved for __ __ __. |
|
Definition
- Eptifibatide and Tirofiban
- acute coronary syndrome |
|
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Term
| Cilostazol inhibits ___ which increases ___. This inhibits __ __ and causes ___. This is used to reduce symptoms of ___. It is contraindicted in pts with __. |
|
Definition
- inhibits PDE III
- increases cAMP
- inhibits platelet aggregation
- vasodilation
- claudication
- CI in CHF |
|
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Term
| Drug used for claudication symptoms? |
|
Definition
Cilostazol (Pletal)
Pentoxyfylline (Trental) |
|
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Term
| CI to Cilostazol (Pletal) |
|
Definition
|
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Term
| Pentoxifylline (Trental) is a __ __ that __ __ __ via enhancing __ __ which __ __ __. It may also decrease __ levels and increase __ levels. |
|
Definition
- hemorrheologic agent
- improves blood flow
- enhancing RBC flexibility
- decreases blood viscosity
- decrease TXAs and increase PGI2 |
|
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Term
| Indications for Pentoxyfylline |
|
Definition
intermittent claudication
chronic occlusive arterial disease of the limbs |
|
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Term
| Drug indicated for chronic occlusive arterial disease of the limbs? |
|
Definition
| Pentoxyfyllline (Trental) |
|
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Term
| CI to Pentoxyfylline (Trental): |
|
Definition
|
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Term
| AntiCOAGULANTS are primarily used for: |
|
Definition
- acute MI
- acute peripheral vascular disease occlusion
- stroke prophylaxis |
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Term
|
Definition
- Heparin
- Low MW Heparin
- Warfarin |
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Term
| Side effects of anticoagulants: |
|
Definition
|
|
Term
| Heparin must be given __ in the __. It has a __ onset. |
|
Definition
- parenterally
- hospital
- fast |
|
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Term
| Warfarin is __, __ patient, and has a __ onset. |
|
Definition
- oral
- out-patient
- slow |
|
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Term
|
Definition
- prophylaxis of post-op thrombosis
- MI
- unstable angina
- deep venous thrombosis
- pulmonary embolus
- extra-corporeal circulation (hemodialysis or heart-lung machine)
- disseminated intravascular coagulation (DIC)
- TIA- probably effective but very risky, not used if stroke in progress |
|
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Term
| Heparin can result in __ and __. With long term administration it can cause ___. |
|
Definition
- DIC
- HIT (heparin induced thrombocytopenia)
- osteoporosis |
|
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Term
| Heparin overdose can result in hemorrhage. ___ at site of infection may occur. __ and __ are rare side effects that may occur. |
|
Definition
- Hematoma
- Alopecia and priapism |
|
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Term
|
Definition
- any site of active or potential bleeding
- severe hypertension
- vascular aneurysm
- recent head, eye, or spinal cord surgery
- head trauma
- lumbar puncture
- regional anesthetic block
- tuberculosis
- visceral carcinoma
- GI ulcers |
|
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Term
| most common drug induced thrombocytopenia: |
|
Definition
| HIT (look for drop in platelets less than 100,000) |
|
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Term
|
Definition
- Type I Non-immune HIT
- Type II Immune Mediated HIT (potentially serious) |
|
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Term
| How do you monitor heparin therapy? |
|
Definition
- aPTT tested prior to starting therapy
- aPTT of 1.5-2.0 times control is the typical therapeutic goal |
|
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Term
| Heparin overdose management? |
|
Definition
1. Stop heparin
2. Protamine sulfate- given IV slowly, binds to and inactivates heparin
3. Fresh frozen plasma |
|
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Term
| Low molecular weight heparins: |
|
Definition
- ENOXAPARIN
- Dalteparin
- Ardeparin
- Danaparoid |
|
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Term
| Low MW heparins are __ __ pieces of regular heparin. They have greater ___ __ activity and less ____ activity. |
|
Definition
- smaller active
- greater anti-Xa activty
- less anti-platelet activity |
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Term
|
Definition
- s.c. injection for prophylaxis for DVT associated with hip, knee, and abdominal surgery
- longer duration, simple kinetics, clotting tests not required |
|
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Term
| For patients on heparin, you want the INR between __ and __, unless they have mechanical heart valves in which case you want it between __ and __. |
|
Definition
|
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Term
| Warfarin (Coumadin) is an oral anticoagulant that inhibits __ __ __ __ thereby inhibiting __ __ ______ ___ of clotting factors: thrombin, VII, IX, X, and protein C and S. Without the addition of the gamma carboxyglutamic acid residue, the clotting factors cannot bind calcium and are inactive. |
|
Definition
- vitamin K epoxide reductase
- vitamin K dependent post translational modification |
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Term
| Warfarin inhibitis vitamin K reductase. Also changes protein C and S which are natural anti-coagulants. So when you first give warfarin there is a tendency to hypercoagulability. |
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Definition
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Term
| Warfarin has a __ onset of __ hours. The __ onset is due to the __ __ __ of warfarin and the fact that preexisting clotting factors are slowly cleared from the blood. It has a __ duration of __ to __. |
|
Definition
- delayed
- 36-72 hours
- delayed
- long half life
- prolonged duration
- 25-60 hours
TAKES 5 TO 7 DAYS OF WARFARIN TO REACH A STEADY STATE |
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Term
|
Definition
- overlap with heparin to avoid long delay in onset
- deep venous thrombosis
- pulmonary embolism
- atrial fibriliation
- rheumatic heart disease
- mechanical heart valves |
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Term
Drugs that compete for with Warfarin for p450 cause INR to go up.
The lower the INR, the greater risk of coagulation. |
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Definition
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Term
|
Definition
| - PREGNANCY- teratogen, fetal hemorrhage |
|
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Term
|
Definition
- situations where the risk of hemorrhage is greater than the potential benefits
- uncontrolled alcohol/drug abuse
- unsupervised dementia/psychosis
- increased risk of falls- elderly, movement disorders |
|
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Term
| The goal of THROMBOLYTIC therapy is to dissolve __ __ by injecting a __ __ or an __ of endogenous fibrinolysis without causing __ ___. |
|
Definition
- pathological clots
- fibrinolytic enzyme
- activator
- without causing uncontrolled bleeding |
|
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Term
| Desirable qualities of anti-coagulants: |
|
Definition
As or more effective than current agents
As or safer than current agents
Oral
Fixed dosing
Minimal food and drug interactions
Predictable anticoagulant response (no monitoring)
Rapid onset and offset of action
Reversible |
|
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Term
| Indirect thrombin inhibitors are __ and __. An oral direct thrombin inhibitor is ___. |
|
Definition
- heparin and LMWH
- Dabigatran |
|
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Term
| 4 advantages and mechanisms of direct thrombin inhibitors over indirect thrombin inhibitors: |
|
Definition
1. better suppression of thrombus growth via inhibiting free and bound thrombin
2. retain activity in presence of platelet rich thrombi b/c do not bind PF4 or vWF
3. predictable anticoagulant response b/c do not bind plasma proteins
4. no risk of HIT |
|
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Term
| Dabigatran is an ___ and __ __ __. |
|
Definition
- anticoagulant
- direct thrombin inhibitor |
|
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Term
| Dabigatran FDA approved for: |
|
Definition
| - prevention of stroke and systemic embolism in NON-VALVULAR ATRIAL FIBRILLATION |
|
|
Term
| Dabigatran etexilate is a new __ __ __ __ __. It is a ___ that is converted to __. |
|
Definition
- reversible oral direct thrombin inhibitor
- prodrug
- dabigatran |
|
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Term
|
Definition
- binds clot bound and free thrombin with high affinity and specificity
- no liver metab
- 80% renal excretion
- predicable anticoag effect
- fixed dose
- no need for monitoring
- no liver toxicity
- no interaction with food
- no interaction with CYP450 |
|
|
Term
Dabigatran:
Administration
Can be taken with or without food
Up to 1/3 of pts complain of GI side effects, suggest to take with food
MUST be swallowed whole
MUST keep in blister pack or original bottle
If bottle, only good for 30 days after opening bottle
Cannot place into pill boxes or prescription bottles |
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Definition
|
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Term
|
Definition
| 13 hours (longer with renal failure) |
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Term
| Dabigatran drug interactions: |
|
Definition
- No CYP450 interactions
- do NOT give with Rifampin |
|
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Term
|
Definition
Antidote
None
Supportive care, blood products, FFP, factor VIIa
No role for vitamin K or protamine
Cost
AWP: $243 per month ($4.05 per capsule)
Verify insurance coverage before starting or discharging a patient on dabigatran |
|
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Term
|
Definition
Alternative to warfarin for prevention of stroke in patients with non-valvular atrial fibrilation
MUST take whole, consider taking with food
MUST store in original packaging
Monitor for bleeding, GI upset |
|
|
Term
| What are the two ARBs approved for heart failure? |
|
Definition
|
|
Term
| Antihypertensive drug list: |
|
Definition
α-adrenoceptor antagonists: prazosin, tamsulosin, terazosin
nonspecific β-adrenoceptor antagonists: carvedilol, propranolol
β1-adrenoceptor antagonists: atenolol, metoprolol succinate and metoprolol tartrate
Calcium channel blockers: amlodipine, felodipine, nifedipine
ACE-Is: lisinopril, ramipril
ARBs: candesartan, valsartan, losartan, olmesartan
Centrally acting antihypertensives: clonidine, methyldopa
Other antihypertensives: minoxidil, hydralazine, nitroprusside, felodapam, |
|
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Term
| Most common side effect of all antihypertensive drugs: |
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Definition
|
|
Term
|
Definition
- Furosemide
- Bumetanide
- Torsemide |
|
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Term
| Pt has bp of 140/90, what do you do? Start with lifestyle changes and document bp over a few times. Exercise, low sodium diet low fat diet. Find bp to be up on 3 diff occassions, which is the first antihtn drug you give? HCTZ (KNOW THIS). It prob won’t work, but it might. Next drug to give? ACE-I (KNOW THIS). Typically lisinopril (ACE-I), can also do Captopril (unique in that it has short duration). ACE-I can cause cough (common), angioedema (severe). Ramopril is another ACE-I- it is better penetrating, called a tissue-ACE-I. Pt gets angioedema (swelling of face areas)> take off ACE-I. Put them on ARB= sartans, 2 sartans for heart failure in place of ACE-I: Candesartan and Valsartan (KNOW THESE TWO), still at higher risk for angioedema but worth the risk b/c so effective against heart failure. |
|
Definition
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Term
| What type of diuretic is most commonly used for HTN? |
|
Definition
|
|
Term
|
Definition
- HCTZ (hydrochlorthiazide)
- Chlorothiazide
- Cyclothiazide
- Metolazone- works in distal convoluted tubule like thiazides, but not thiazide in structure |
|
|
Term
| Thiazide diuretics work on the __ __ _. |
|
Definition
|
|
Term
| Potassium sparing diuretics: |
|
Definition
- Spriranolactone
- Triamterene
- Amiloride |
|
|
Term
| HCTZ tends to __ blood __. |
|
Definition
|
|
Term
| Diuretics electrolyte possible side effects: |
|
Definition
| - electrolyte imbalance (HYPOKALEMIA MOST COMMON, then hyperkalemia, can also include calcium imbalance, hypomagnesium, and hyponatremia) |
|
|
Term
|
Definition
- electrolyte imbalance
- hyperlipidemia
- glucose intolerance, insulin resistance
- hyperuricemia
- rare> nephritis, blood dyscrasias, cholecystitis, pancreatitis, necrotizing vasculitis |
|
|
Term
| Furosemide most likely to cause hypokalemia but may also occur with HCTZ. The other electrolyte imbalance that may occur is hyponatremia |
|
Definition
| Loop (furosemide) likely to cause hypokalemia, HCTZ can too |
|
|
Term
| Adrenergic blockers can be central acting or post-synaptic alpha receptor blockers. |
|
Definition
|
|
Term
| Central acting adrenergic blockers: |
|
Definition
- Clonidine
- Methyldopa
- Guanabenz
- Guanfacine |
|
|
Term
| Central acting adrenergic blockers work by __ ___ __. These lower sympathetic activity allowing for a modest decrease in __ __ __, __ __ and __ ___. |
|
Definition
- blocking adrenergic transmission
- peripheral vascular resistance
- cardiac output
- renin levels |
|
|
Term
| Side effects of central acting adrenergic blockers: |
|
Definition
- sedation
- dry mouth
- rebound HTN
- fluid retention |
|
|
Term
| Alpha 1 blockers are selective post synaptic catecholamine blockers. They decrease __ __ __ and __. |
|
Definition
- peripheral vascular resistance
- preload |
|
|
Term
|
Definition
- Doxazosin
- Prazosin
- Terazosin |
|
|
Term
| Side effects of alpha 1 blockers: |
|
Definition
- first dose hypotension response
- headache
- drowsiness
- fatigue
- dizziness
- asthma type response |
|
|
Term
| Alpha 1 blockers not used much for bp control, but may be used for BPH. These blcok symptahtetic outflow at terminal end: block NE on alpha 1 receptors on the vascular smooth muscle, primarily on the small resistance vessels. (only place epi comes from in body is adrenal glands) |
|
Definition
|
|
Term
| Clonidine: used in pts with really difficult to control HTN, activates alpha 2 receptors in the brainstem which results in decreased sympathetic output, very short acting, has to be given 3 times a day, can also be given as patch to slowly release it, big side effect: rebound HTN, dry mouth, also causes sleepiness (Guanavine and ___ work same way), NOT GIVEN IN HEART FAILURE B/C CAN CAUSE FLUID RETENTION |
|
Definition
|
|
Term
| Beta blockers reduce __, __, __ release, __ __ __, and __ release. |
|
Definition
- CO
- HR
- renin release
- peripheral vascular resistance
- catecholamine release |
|
|
Term
|
Definition
- Atenolol
- Metoprolol
- Propanolol
- Bisoprolol
- Nebivolol |
|
|
Term
| Propanolol blocks beta 1 and 2 receptors. What beta receptors only block beta 1 receptors? |
|
Definition
|
|
Term
| What beta blocker is not very good for HTN but used frequently for CHF? |
|
Definition
|
|
Term
| Beta blocker side effects: |
|
Definition
- hypotension
- bradycardia
- insomnia
- depressed mood
- night mares
- sexual dysfunction
- hypoglycemia
- dislipidemia (lowers HDL, raises TG)
- bronchospasm |
|
|
Term
| Combined alpha and beta blockers: |
|
Definition
|
|
Term
| Combined alpha and beta blockers work by decreasing __ and __. |
|
Definition
|
|
Term
| Side effects of combined alpha and beta blockers: |
|
Definition
- orthostatic hypotension
- much less cns side effects as well as lipid/glycemic/pulmonary effects |
|
|
Term
|
Definition
- Hydralazine
- Minoxidil
- Nitroglycerin
- Nitroprusside |
|
|
Term
| Hydralazine side effects: |
|
Definition
lupus symptoms
tachycardia |
|
|
Term
|
Definition
hirsutism
pericardial effusion |
|
|
Term
| Calcium channel blockers decrease the inotropic effect, meaning they decrease ___. |
|
Definition
|
|
Term
| Non-dihydrapyridine calcium channel blockers: |
|
Definition
- Verapamil
- Diltiazem
(NVD) |
|
|
Term
|
Definition
- Nifedipine
- Amlodipine
- Felodipine |
|
|
Term
amiloride- potassium sparing diuretic
amlodipine- dihydropyridine CCB
amiodarone- potassium channel blocker |
|
Definition
|
|
Term
| Side effects of caclium channel blockers: |
|
Definition
- ankle edema
- headaches
- flushing
- gingival hyperplasia (dihydorpyridines) |
|
|
Term
| Main categories of Vasodilators: |
|
Definition
- Direct Vasodilators: Hydralazine, Minoxidil, Nitroglycerin, Nitroprusside
- CCB
- ACE-I
- ARBs (angiotensin II receptor blockers)
- Direct renin inhibitors |
|
|
Term
| ACE-I inhibit ___ __ and increase __ levels. |
|
Definition
|
|
Term
|
Definition
- Captopril
- Ramipril
- Enalapril
- Lisinopril
- Quinapril
- Benazepril |
|
|
Term
|
Definition
- dry hacking cough
- angioedema
- rash
- first dose hypotension
- hyperkalemia
- caution with increasing renal insufficiency |
|
|
Term
|
Definition
- predictable, mild, dose related side effects
- blunts hypokalemia caused by diuretics
- little orthostatic hypotension or SNS activation
- no effect on TGs or cholesterol |
|
|
Term
|
Definition
| 2nd and 3rd trimester pregnancy |
|
|
Term
|
Definition
Initial dose hypotension problem, esp. if hypovolemic
Skin rashes/neutropenia (is captopril worse than others?)
Acute renal failure in renal artery stenosis
African-Americans and elderly may not respond well
Hyperkalemia possible (esp. if combined with other drugs that increase K+) |
|
|
Term
| what populations don't respond well to ACE-I? |
|
Definition
- African Americans
- elderly |
|
|
Term
|
Definition
- Losartan
- Valsartan
- Olmesartan
- Candesartan
- Irbesartan |
|
|
Term
|
Definition
- hyperkalemia
- angioedema
- first dose hypotension
- caution with increasing renal insufficiency |
|
|
Term
|
Definition
|
|
Term
| Aliskiren (direct renin inhibitor) side effects: |
|
Definition
- diarrhea
- angioedema
- rash |
|
|
Term
|
Definition
Block AT1 subtype of the AT II receptors
Effects, uses and side-effects similar to ACE inhibitors (remember that side-effects of ACE-I are relatively benign)
In contrast to ACE-I, no cough with ARBs
Less chance of angioedema
Avoid during pregnancy
ACE inhibitors generally prescribed first |
|
|
Term
| AA tend to respond well the ___, but not to __ or __. |
|
Definition
- well to HCTZ
- not to ACE-I or beta blockers |
|
|
Term
| General approach to antihtn meds: |
|
Definition
General approach
Thiazides
ACE-I - ATII blockers (ARBS)
Beta blockers
Calcium channel blockers
Alpha blockers
Vasodilators |
|
|
Term
| POST MI: BETA BLOCKERS AND ACE-I ARE USED EVEN IF DON’T HAVE HTN. |
|
Definition
|
|
Term
| A 48-year-old male reports that he has experienced chest pain on several recent occasions. These pains are described as a squeezing sensation with a substernal location. He was physically active just before each of the attacks. For example, his most recent episode occurred when he was mowing his yard on a hot summer day. A few minutes of rest relieves the attacks. His blood pressure is 144/93 mmHg at rest and pulse is 78 beats/min. An exercise stress test with ECG reveals depressed ST segments during exercise consistent with myocardial ischemia and EF = 60% (normal). Which of the following agents would be preferred for chronic, stable angina in this patient and without heart failure? |
|
Definition
- Metoprolol tartrate
or
- Isosorbide dinitrate |
|
|
Term
| Do NOT stop __ or __ __ abruptly b/c rebound HTN may occur. |
|
Definition
- clonidine
- beta blockers |
|
|
Term
| __ can cause respiratory depression. |
|
Definition
|
|
Term
| TGs at 600, treat with a Fenofibrate like Gemfibrozol KNOW THIS. |
|
Definition
|
|
Term
| BETA BLOCKERS AREN’T PREFERRED FOR DIABETICS BC MASKS SYMPTOMS. HCTZ NOT USED B/C INCREASES GLUCOSE. USE ACE-I ON DIABETIC PT WITH HTN. |
|
Definition
|
|
Term
| Mechanisms that may reduce bp: reduced CO, increased vagus nerve activity (acetylchline on muscarinic receptors), decreased central sympathetic outflow, reduced angiotension II levels. |
|
Definition
|
|
Term
| How do you reduce angiotension II levels? Not ARBs, yes ACE-I would . |
|
Definition
|
|
Term
| ACE-I DO NOT CAUSE ORTHOSTATIC HYPOTENSION. |
|
Definition
|
|
Term
| WHAT ANTIHTN MED INHIBITS PEPTIDYL DIPEPTIDASE: ACE-I DO. |
|
Definition
|
|
Term
| Sstellate ganglion: star shaped ganalion that goes to the heart. It’s the Sympathetic outflow to the heart. Decrease contractility. |
|
Definition
|
|
Term
| Categories of anti-angina drugs: |
|
Definition
1. Nitrates
2. Beta blockers
3. Calcium channel blockers
4. Late Sodium Blocker |
|
|
Term
Nitrates
Primary Action(s) – Vasodilates coronary arteries
Given oral, sublingual, IV, topically
Given urgently and chronically |
|
Definition
|
|
Term
| Beta blockers can relieve angina by decreasing myocardial __ demand by decreasing __ __, __ __, and ___. These can be given __ and __. Usually used in chronic managment, but can be used urgently. |
|
Definition
- oxygen
- blood pressure
- heart rate
- contractility
- IV and orally |
|
|
Term
| Calcium channel blockers can relieve angina by reducing myocardial __ __, ___, and __. |
|
Definition
- oxygen consumption
- preload
- afterload |
|
|
Term
| __ is a late sodium blocker used to relieve angina symptoms. Its primary action is to decrease __ __ and increase __ ___. Used after other anti-angina drugs have failed, may be used with beta blocker, nitrates, calcium channel blockers, antiplatelets, lipid lowering therapy, ACE-I, and ARBs. |
|
Definition
- Ranolazine (Renexa)
- myocardial stress
- increase myocardial perfusion |
|
|
Term
| Dislipidemia medications: |
|
Definition
- HMG-CoA reductase inhibitors
- Bile Acid Sequestrants
- Fibric Acids
- Nicotinic Acids
- Cholesterol Absorption Inhibitors
- Omega 3 Fatty Acids |
|
|
Term
| HMG-CoA reductase inhibitors (statins) enhance __ __ ___ and increase ___ clearing from the plasma. What are they used for? |
|
Definition
- hepatocyte LDL receptors
- increase LDL clearing
- used for increased LDL, modest effect on trigs, very little effect on low HDL |
|
|
Term
| Side effects of HMG CoA reductase inhibitors: |
|
Definition
- myopathy
- rhabdomyolysis
- increased liver enzymes |
|
|
Term
| HmG CoA reductase inhibitors: |
|
Definition
- Atorvastatin
- Rosuvastatin
- Simvastatin
- Pravastatin
- Lovastatin |
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Term
| Bile acid sequestrants work in the __ to increase __ __ and __ __ in the bile. |
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Definition
- liver
- LDL clearance and cholesterol loss |
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Term
| Bile Acid Sequestrant uses: |
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Definition
- high LDL
does not improve and may increase TGs |
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Term
|
Definition
- Cholestyramine
- Colestipol
- Colesevelam |
|
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Term
| Side effects of bile acid sequestrants: |
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Definition
GI distress
constipation
decreased absorption of other drugs |
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Term
| Fibric acids enhance __ __ in the __ ___ and improve removal of ___. |
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Definition
- lipoprotein lipase
- peripheral tissues
- removal of TGs |
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Term
|
Definition
| - high TGs, good effect on LDL, modest effect on low HDL |
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Term
|
Definition
- Gemfibrozil
- Fenofibrate
- Clofibrate |
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Term
| Fibric Acid side effects: |
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Definition
- dyspepsia
- gallstones
- myopathy
- rhabdomyolysis |
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Term
| Nicotinic Acid limits __ __ __ from __ __ which decreases __ release of __. |
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Definition
- limits free fatty acids from adipose tissue
- decreases hepatic release of VLDL |
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Term
|
Definition
| Primarily elevates HDL, high modest lowering of LDL and Apo B, low modest effect on increased TGY |
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|
Term
|
Definition
|
|
Term
| Nicotinic acid side effects: |
|
Definition
- flushing
- hyperglycemia
- hyperuricemia
- UGI distress
- hepatotoxicity |
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Term
| Cholesterol Absorption Inhibitors decrease cholesterol absorption in the gut. One such drug is: |
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Definition
|
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Term
| Uses of cholesterol absorption inhibitors (Ezetimibe): |
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Definition
| - high LDL, no substantial effects on HDL or TG |
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Term
| Side effects of Ezetimibe (cholesterol absorption inhibitor) |
|
Definition
- arthralgias
- back pain
- abdominal pain
- diarrhea
- cough |
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Term
| Omega 3 fatty acids reduce the production of __ and remnants. |
|
Definition
|
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Term
|
Definition
| - used for high TG, but modest effects on LDL and HDL |
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Term
| Omega 3 fatty acid side effects: |
|
Definition
- eructation
- infection
- flu like symptoms
- dyspepsia
- taste changes
- back pain |
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Term
| Cannot give Cerivastatin with _____. |
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Definition
|
|
Term
| Statin least likely to have drug interactions: |
|
Definition
|
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Term
|
Definition
With 2 risks, e.g., ischemic disease and diabetes, “optional” goal is to reduce LDL<70 mg/dL (desirable without risk factors is <130)
Recent data have shown a 25% reduction in stroke (no reduction in brain hemorrhage) in at risk populations |
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Term
|
Definition
Numerous, but incidence is low and severity is relatively lesser than with other lipid lowering drugs
Most frequent is hepatic damage (1-2%). Elevated serum hepatic enzymes occur, and they can cause hepatitis
Monitor liver enzymes after 1-2 months and then every 6 months
Contraindicated in hepatic disease
Increasing number of reports of peripheral neuropathies. Appear reversible on discontinuation of the drugs
Watch for myalgia, myopathy (<1%) and rhabdomyolysis (rare).
Monitor more carefully when combining with niacin (2%) or fibrate drugs (5%), which can cause the same toxicity). These toxicities occur more frequently.
Avoid combining with erythromycin (dec. metabolism of statins, with inc. myopathy) |
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Term
| Monitor for rhabdomyolysis carefully when combining statins with __ or __ drugs. |
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Definition
|
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Term
| 3 drugs that can cause rhabdomyolysis |
|
Definition
fibrate drugs
niacin
statins |
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Term
| Avoid combining statins with ___ b/c this drug decreases metebolism of statins increasing myopathies. |
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Definition
|
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Term
| what do you monitor to look for rhabdomyolysis? |
|
Definition
creatine phosphokinase (CPK aka CK)
Mechanism is not entirely clear
HMG-CoA inhibitors also inhibit Q10, and this mechanism is most likely |
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Term
|
Definition
Itching, flushing and unpleasant sensation of being warm.
Prostaglandin mediated.
Give aspirin (blunts, but does not remove, this effect).
G.I. distress (may activate ulcers)
Inhibits urate secretion. Hyperuricemia in 20% of pts.
Hepatotoxicity
Severe is rare, and reversible
Occurs mostly with older sustained release forms
Monitor liver fx regularly
Liver injury is less likely with Niaspan® (given once daily) the new extended release formulation
Carbohydrate tolerance may be moderately impaired (hyperglycemia)
Reversible
Can still be given to diabetics receiving insulin |
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Term
| Gemfibrozil (Lopid) is used to reduce ___ when __ is high or when __ is elevated. |
|
Definition
- triglycerides
- VLDL
- IDL |
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|
Term
Reduction of triglycerides when VLDL is very high, or when IDL is elevated
Follow VLDL. If it is elevated, gemfibrozil is a candidate drug. If LDL is elevated but VLDL is not elevated, do not use this drug. |
|
Definition
| Gemfibrozil or Fenofibrate |
|
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Term
|
Definition
Blood cell deficiencies, skin rash and other hypersensitive rx
g.i. problems
liver enzyme abnormalities (usually transient)
myositis -- myopathy and rhabdomyolysis are reported when combined with HMG-CoA reductase inhibitors
lithiasis ( biliary cholesterol excretion). Do NOT use in pts with gall bladder problems. |
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Term
| Cholestyramine (Questran) Colestipol (Colestid) Colesevelam (Welchol) |
|
Definition
Enhanced excretion of bile acids, leading to conversion of cholesterol to bile acids in the liver.
Loss of cholesterol triggers up regulation of LDL receptors in the liver: therefore, LDL |
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Term
|
Definition
Inhibits absorption of phytosterols and cholesterol
Primarily useful for reducing LDL cholesterol
Decreases cholesterol absorption approx 50%
Does not modify triglyceride absorption
Often used in combination with a statin |
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Term
| Classes of Antiarrhytmic drugs; |
|
Definition
Some Block Potassium Channels.
1. Sodium Channel blockers
2. Beta Blockers
3. Potassium channel blockers
4. Calcium channel blockers |
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Term
| 2 other anti-arrhythmic drugs: |
|
Definition
Adenosine SA and AV node agonist
Used primarily for PSVT
Side effects – Bronchospasm, hypotension, may invoke tachycardia in WPW
Digitalis Slows AV node conduction
Used primarily in PSVT and Atrial Fibrillation
May invoke tachycardia in WPW, can be toxic |
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Term
| Side effects of potassium channel blockers (amiodarone): |
|
Definition
- vision changes
- bluish skin
- pulmonary fibrosis
- thyroid changes |
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|
Term
|
Definition
First Line Agents
Diuretics
Typically Loop Diuretics
If wet Diurese
Beta Blockers (Don’t start or increase if wet)
Carvidelol
Metoprolol XL
ACEI/ARB
Other Agents
Nitrates
Spironolactone
Digoxin
Hydralazine/Isosorbide
Amlodipine |
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Term
| DIG AND FUROSEMIDE DON’T BENEFIT MORTALITY, SRICTLY FOR SYMPTOMS. |
|
Definition
|
|
Term
Digoxin is the only oral inotrope and is a weak inotrope at best. Use is primarily useful in heart failure but is controversial.
IV Inotropes Used primarily in left ventricular dysfunction such as in acute and chronic heart failure.
Medications – Dobutamine, Dopamine |
|
Definition
|
|
Term
Dopamine helps stimulate the heart and keeps the kidney vessels open so kidneys stay profused.
NE (levophed) used in severe shock to cause vasoconstriction on alpha receptors. |
|
Definition
|
|
Term
|
Definition
Tx of hypertension
Tx of fluid retention - such as
CHF
renal disease (CRF)
hepatic cirrhosis
Carbonic anhydrase inhibitors
Thiazides
Loop diuretics
Potassium-sparing diuretics
Osmotic diuretics |
|
|
Term
| Carbonic Anhydrase Inhibitors: |
|
Definition
- prevent formation of H+ and HCO3-
- less H+ to exchange for Na+
- less Na+ reabsorbed
- water follows sodium so less water resabsorbed |
|
|
Term
| adverse effects of carbonic anhydrase inhibtors: |
|
Definition
|
|
Term
| Mannitol is an __ __ that is freely filtered, non-reabsorbable, and non-metabolized. Urea, glycerin, and isosorbide are less effecient and can penetrate membranes. |
|
Definition
|
|
Term
|
Definition
1. acute renal failure to maintain urine flow
2. reduce CSF volume and pressure- often used after head injury
3. hemodialysis to facilitate excretion of toxic substances |
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|
Term
Loop diuretics
Prototype: Furosemide (Lasix®)
Oral absorption: diuresis begins in 30-60 minutes and persists for 8 hours
I.V. administration: diuresis begins within 5 minutes and persists for 2 hours. With I.M. administration, diuresis begins in 30 minutes
Usual dosages:
Oral – 20-80mg/dose QAM-BID. Max: 600mg/day
Acute pulmonary edema: 40mg I.V. infuse over 1-2 minutes |
|
Definition
|
|
Term
Loop diuretics
Bumetanide (Bumex®) (PO, I.M., I.V.)
Usual oral dosage for edema: 0.5-2mg/dose QD-BID. Max: 10mg/day
Torsemide (Demadex®) (PO, I.V.)
Usual dosage for CHF or CRF: 20mgQD
Usual dosage for HTN or hepatic cirrhosis: 5-10mgQD |
|
Definition
|
|
Term
| Indications for a loop diuretic: |
|
Definition
1. Edema of cardiac, hepatic, or renal origin
2. Acute pulmonary edema associated with CHF
3. HTN that cannot be controlled with other diuretics
4. Acute renal failure
5. Hypercalcemia- loops can increase excretion of calcium in the urine |
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|
Term
| Thiazide diuretics have a ___ structure. They all can be given orally. HCTZ has a half life of __ hours whereas the others have a half life of __ hours. All of them are actively secreted in the __ __ __. |
|
Definition
- sulfonamide
- 12
- 24
- distal convoluted tubule |
|
|
Term
, metolazone - “thiazide-like”
These agents work at the same site as thiazides but have different structures. When loop diuretics fail, these agent may serve as a adjunct with the loop diuretic to produce diuresis. |
|
Definition
|
|
Term
|
Definition
1. HTN (10-15 mm Hg max fall in arterial pressure)
reduce blood volume (volume returns to near normal over 6-8 weeks, but antihypertensive effect remains)
reduce vascular resistance by relaxation of arterioles (Na+ increases vessel stiffness, so reducing Na+ relaxes arterioles)
reduce responsiveness of arterioles to NE (also because of lower Na+) |
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|
Term
| Thiazides adverse effects: |
|
Definition
1. Hypokalemia (esp watch with digoxin)
2. Hypercalcemia
3. Hyponatremia with hypovolemia
Hyperglycemia (decrease insulin secretion -- may unmask latent diabetes mellitus)
Erectile dysfunction
Frequency is even greater than with beta-blockers
Increased serum cholesterol – usually clinically important only at high dose
Allergic reactions |
|
|
Term
Spiranolactone – steroid
Site of Action: cortical collecting duct
Mechanism: competes for the aldosterone receptor
Pharmacokinetics: Can take between 10-48 hours to start working.
Why? |
|
Definition
Not very efficacious as diuretics by themselves at least at normally used doses.
By this point in the transit of Na+ in the kidney, there isn’t very much left
Used to prevent K+ loss
Counteract this side-effect of thiazides and loops
Hyperaldosteronism syndromes (rare occurrence) |
|
|
Term
| potassium sparing diuretics and the heart: |
|
Definition
There are mineralocorticoid receptors in the heart as well
Local production of aldosterone in the heart is proportional to degree of heart failure
Aldosterone may stimulate cardiac fibrosis and hypertrophy (Bad)
Spironolactone and eplerenone have been shown to be useful in the long term management of heart failure. (we’ll discuss more in the CVS lectures) |
|
|
Term
| potassium sparing diuretic SEs: |
|
Definition
Spiranolactone
Hyperkalemia (esp. with ACE inhibitors, NSAIDs)
Most common when co-administered with K+ supplement or patients that eat too much K+ rich food.
Anti-androgen effect (steroid structure leads to competitive inhibition of androgen receptors)
gynecomastia; impotence |
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