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176 Cards in this Set
- Front
- Back
- 3rd side (hint)
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classes of receptors
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Ligand gated ion channels
G protein coupled receptors Enzyme linked receptors Intracellular receptors |
Intracellular receptors induce transcription
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Drug metabolism phases
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Phase 1:oxydation
Phase 2: Conjugation |
1 usually renders drug inactive
2 increases soluability for fecal (by congugation) or renal (polar species) elimination. |
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CYP3A inducers
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St. Cohns Wort
Carbamazapine Rifampin Rifabutin Ritanovir |
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CYP3A inhibitors
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Grapefruit juice
-conazoles -omyacins cimetidine Ca channel blockers, statins, versed, Hg |
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Cyp 1A2 inducers
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smoking
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Cyp 1A2 inhibitors
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flouroquinolones
Cimetidine |
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-lol
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beta blocker
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-pril
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Ace inhibitor
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-sin
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Alpha blocker
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-sartin
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Angiotensin receptor blocker (ARBS)
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-pine
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Cancium channel blocker
(exceptr verapamil and diltiazem) |
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Thizaide
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Reduce Na+ & H2O
-lowers blood volume -lowers CO -Lowers peripheral resistance (watch for Hypokalemia, hyperglycemia and increased lipids, and uricemia) |
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Loop diuretics
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Lasix , Ethacrynic acid
( hypo k,Mg, OTOTOXICITY hyperuricemia, decreased renal function) Potentiated by anminoglycoside antibiotics |
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4 ways to treat hypertension
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lower blood volume
sympathectomy ( alpha 1, beta 1) Vasodilate Reduce renin anngiotensin aldosterone system |
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4 types of beta blockers
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non selective
selective combined beta and alpha 1 blocker/partial agonist |
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Non-selective B blockers
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propranolol (inderol)
Nadolol (corgard) |
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Selective B blocker
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B1>>B2
metoprolol (lopressor) Atenolol (tenormin) |
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Combined B blocker
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B1 and 2 and Alpha 1
Labetalol (normodyne) Carvedilol (coreg) |
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B Blocker with ISA
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ISA=intrinsic sympathomimetic activity
Acebutolol Pindolol - for htn in diabetics or slow heart rate. |
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Nebivolol
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Strongly selective B blocker with Vasodilatory effect via Nitric oxide release
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Selective B blocker
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B1>>B2
metoprolol (lopressor) Atenolol (tenormin) |
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B blocker adverse effects
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Arrhythmias
CNS (fatigue, Insomnia, Hallucinations) ED, Bronchospasm (wih non selective) Metabolic |
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Combined B blocker
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B1 and 2 and Alpha 1
Labetalol (normodyne) Carvedilol (coreg) |
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B Blocker with ISA
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ISA=intrinsic sympathomimetic activity
Acebutolol Pindolol - for htn in diabetics or slow heart rate. |
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Nebivolol
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Strongly selective B blocker with Vasodilatory effect via Nitric oxide release
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B blocker adverse effects
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Arrhythmias
CNS (fatigue, Insomnia, Hallucinations) ED, Bronchospasm (wih non selective) Metabolic (lowers HDL, hypoglycemia , DM type II in elderly) |
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B blocker indication
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HTN in CHF and recent MI pts.
Some ISA and Nitric oxide B blockers may be first tier for htn tx. |
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Alpha 1 blockers
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Doxazosin prazosin terazosin
Lower art. and vev. resistance min changes in cardiac output or renal function. Relaxes bladder sphincter Careful with first dose, can have reflex tachycardia, postrual syncope |
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Alpha 2 agonist
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Clonadine
centrally reduces blood pressure (sympathoplegic) -stops hot flashes |
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Alpha 2 agonist
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cAlpha methyldopa
centrally reduces blood pressure reducing adrenergic outflow from CNS. leads to reduce total peripheral resistnce, Does not effect CO or Renal perfusion. Very helpful for Renal insufficient pt. with htn. May cause sedation Ok for Pregnant pts. |
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Ganglionic blocker
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mecamylamine, Trimethaphan. Emergently used to lower blood pressure.
Reacts specifically on nicotinic receptors of both parasympathetic and sympathetic ganglia, and block all autonomic output from them. |
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Vasodilators
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Hydralazine, Minoxidil
relax vascular smooth muscle (arterioles) get a reflex stimulation of heart, contractility, and heart rate, and o2 consumption, may prompt angina pectoris, or MI. Hydralazine good for PIH. (prgncy htn) -HA Tachycardia, nausea, sweating, arrhythmias Use with dloop diuretic and B blocker. |
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Sodium Nitroprusside
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IV infusion for hypertensive crisis. acts on venous and arterial smooth muscle. (thus can reduce preload)
Half life in minutes. Results in cyanide ion production. Toxicity is ratre bu can be treated with sodium thiosulfate which produces thyanocate which is less toxic and renally eliminated. TOXIC ORALLY |
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Labetalol
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A and B blocker , for Hypertension It is nonselective Beta
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Fenoldopam
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Peripheral dopamine -1 agonist
maintains or increases renal perfusino while lowering blood pressure. contraindicated in glaucoma |
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B blocker indication
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HTN in CHF and recent MI pts.
Some ISA and Nitric oxide B blockers may be first tier for htn tx. |
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Alpha 1 blockers
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Doxazosin prazosin terazosin
Lower art. and vev. resistance min changes in cardiac output or renal function. Relaxes bladder sphincter Careful with first dose, can have reflex tachycardia, postrual syncope |
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Alpha 2 agonist
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Clonadine
centrally reduces blood pressure (sympathoplegic) -stops hot flashes |
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Alpha 2 agonist
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cAlpha methyldopa
centrally reduces blood pressure reducing adrenergic outflow from CNS. leads to reduce total peripheral resistnce, Does not effect CO or Renal perfusion. Very helpful for Renal insufficient pt. with htn. May cause sedation Ok for Pregnant pts. |
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Ganglionic blocker
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mecamylamine, Trimethaphan. Emergently used to lower blood pressure.
Reacts specifically on nicotinic receptors of both parasympathetic and sympathetic ganglia, and block all autonomic output from them. |
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Vasodilators
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Hydralazine, Minoxidil
relax vascular smooth muscle (arterioles) get a reflex stimulation of heart, contractility, and heart rate, and o2 consumption, may prompt angina pectoris, or MI. Hydralazine good for PIH. (prgncy htn) -HA Tachycardia, nausea, sweating, arrhythmias Use with dloop diuretic and B blocker. |
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Labetalol
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A and B blocker , for Hypertension It is nonselective Beta
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Fenoldopam
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Peripheral dopamine -1 agonist
maintains or increases renal perfusino while lowering blood pressure. contraindicated in glaucoma |
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Nicardipine
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Ca channel blocker
Iv infusion 5-15 mg/hr. half life 8 hours. |
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b blocker side effects
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Sexual disfunction
Exercise intolerance |
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Calcium channel blockers classes
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nonselective: Diphenyalkylamines (verapamil
Semi-selective: Benzothazepines (diltiazem) a less negative inotropism Selective Dihydropyridines (nifedipine, nicardipine) |
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CA Channel blockers MOA
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reduce intracellular Ca + lowering arteriole smooth muscle tone. Greater vascular than cardiac effects.
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Ca channel niche
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DM, Asthma, Angina
Intolerance to ACE. |
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Ca channel blockers adverse effects
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Constipation 10%
HA , Dizzy vertigo Fatique Skin rash ( more eczema?) |
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RAA inhibitor classes
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Renin inhibitors
ace inhibitors ARBS (angiotensin receptor blockers) Aldosterone antagonists. |
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ACE MOA
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Stop angiotensin 1 to 2
stop 2 then less aldosterone =decreased blood volume, decreased peripheral resistance |
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Renin inhibitor
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Aliskiren Similar to ACE, may be renoprotective when combined with ARB
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Ace Inhibitor adverse effects
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+K.
cough angioedema TERATOGENIC!! Rash, alters taste |
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ARBS
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Angiotensin receptor blockers
Losartan, valsartan etc. Similar use to ACE, more complete blockade, less cough, more expensive than ace. |
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order of HTN tx
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1 Ace inhibitor, diuretic
2 Arb, B blocker, Ca blocker, Central Sympathoplegic, Alpha blocker |
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HTN drug choices by disease
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DM=ACE, Ca+ channelblockers
CAD= ACE, B blocker Renal= ACE, Vasodilator (Ca+ channel blocker) Renin inhibitor and ARB BPH=alpha blocker. |
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HTN emergency
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BP 210/150
Vasodilators (Ntroprusside, diazoxide) Beta blocker, Dopamine Agonist (fenoldopam) |
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HTN tx drug interference
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NSAIDS, Prostaglandins= vasodilation (important in renal function
Estrogen upregulates angiotensinogen |
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What regulates Na+ homeostasis?
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ADH from Hypothalamus/posterior pituitary holds on to Na.
ANP (atrial naturetic peptide) from heart causes you to loose it. Sympathetic activitiy relaxes the justaglomuleular aparatus allowing the filtrate to flow easier, causing you to loos the Na. Aldosterone increases resorbtion of Na( from renin (kidney) angiotensin (lung) aldosterone (adrenal gland) system). |
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Diuretic drug classes
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Carbonic Anhydrase Inhibitors
Osmotic Agents Loop Agents Thiazide and Thiazide-like Agents Potassium Sparing Antidiuretic hormone (ADH) antagonists |
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Thiazide Diuretics MOA
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Inhibit the Na Cl symport. Results in loss of Na and Cl.
Weakly inhibits Carbonic Anhydrase. Some direct Vascular effects. |
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Thiazide Advers effects
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Hypokalemia
Anorexia, nausea, constipation ED Postural Hypotension CNS: Vertigo, HA, Vision changes. |
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Loop diuretics MOA
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Block Tubule reabsorption of Na+.
Directly dilates veins. Eg: Lasix (furosemide, ethacrynic acid) |
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Loop diruetics Adverse effects
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Ototoxicity (tinnitis, vertigo)
Fluid loss (hypotensions) Electrolyte loss: (K: fatigue, dysrythmia. Cl:alkalosis. Ca: Cramps, tetany. Mg dysrhythmias.) |
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K sparing duretics MOA
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Active at the luminal membrane: (Triamterene, amiloride)
Mineralocorticoid Antagonists: Block Aldosterone.(spironolactione, Eplerenone) Causes loss of Na+ and H2O but holds onto K+ and H+. Primary agent in Cirrhosis, otherwise an adjunct. |
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K sparing duretics Adverse effects
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Gi upset, Ca+ stones, Hyperkalemia (particularly with ACE inhibitors and NSAIDS)
Gynecomastia, Lessen hirsutism in females. Weakly antagonizes Folic Acid |
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Cause and treatment of Pernicious Anemia
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Megaloblastic anemia also,
They are the result of folate deficiency. B 12 if a cofactor in the activation of folate, give Folate for anemia, but no treatment for neurologic damage. and B12 suplementation may or may not be necessary. |
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Problems with EPO
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For most patients with anemia from chronic disease, the risk of death from CVA and MI much greater if Hgb>12.
EPO may act like a growth factor for Cancer. Increases clot risk for major surgery. |
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Clotting cascade (simple)
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Prothrombin converted to thrombin. Thrombin Converts Fibrinogen to Fibrin.
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What breaks up a clot?
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Plasminogen->Plasmin-> degrades fibrin into D-dimer and fibrin split products.
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virchow's triad of thrombosis risk factors
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Hypercoaguable state
Circulatory stasis Endothelial injury |
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Anticoagulant strategies
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1 Block platelets
2 inhibit thrombin directly 3 inhibit thrombin via vitamin k factors 4 inhibit thrombin via antithrombin III |
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Antiplatelet strategies
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Block prostaglandin synthesis
Inhibit ADP from activating platelet. Block platelet receptors (IIb or IIIa) |
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Antiprostaglandin agents
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Aspirin
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Anti ADP indications
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Chronic: prevention of MI and CVA
Acute: coronary stent placement |
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Anti ADP adverse effects
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Nausea Diarrhea (20%) Hemorrhage, Leukopenia
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Warfarin MOA
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Interferes with vitamin K (via NADH) decreases levels of factors II,VII, IX and X
Results in reduced Thrombin levels monitor with Ptt and INR (target 2.5-3.5x normal INR) Metabolized by cytochrome P450 |
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Warfarin Advers effects
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Hemorrhage, Fetotoxic!
Multiple drug interactions rare cutaneous necrosis in early tx. |
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Antithrombin III activators examples and MOA
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Heparin (natural glycosaminoglycan from mast cell) enhances antithrombin III which blocks activation of Factor X. Goal: activated PTT 2-2.5x control
Fondaparinux |
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HIT
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Heparin induced Thrombocytopenia
Type 1: Platelet drop mild Type 2: Immune related seroius drom (>50%) in platelet count. Stop heparin and start another anticoagulant! |
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Thrombolytic drugs
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Streptokinase,
Alteplase Reteplase Anistreplase |
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Reversing Anticoagulation drugs
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Fibrinolytics: Aminocaproic acid
Tranexamic acid Aprotinin Heparin: Protamine Sulfate Warfarin: Vitamin k FFP Prothrombin complex concentrates |
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Atherosclerosis process
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Fatty streak, LDL accumulates under endothelium, monocytes collect in fatty streak, LDL is oxidized, Monocytes become macrophages and ingest LDL and become Foam cells. More LDL accumulates (inflamation!) HDL mitigates this process.
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lipid lowering agents
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Niacin (nicotinic acid)
Bile acid-binding agents Cholestyramine, Colestipol) HMG-CoA reductase inhibitors “Statins”(lovastatin, pravistatin et al) Fibric acid derivatives “Fibrates” (gemfibrozil, fenofibrate) Inhibitors of sterol absorption |
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Statin MOA
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CoA reductase inhibitor
blocks sterol (thus cholesterol) synthesis Lowers risk of CHD proportionallly to fall in LDL |
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Statin Adverse effects
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Gi: nausea, upset
Liver: Elevated enzymes, (monitor transaminases) Myopathy and Rhabdomyolysis (monitor CK levels) increases Warfarin effects. Contraindicated in Pregnant, lcatation, kids, teens |
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statin drug interactions
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cyp450:cyp 3A
Amiodaron & verapamil (myopathy) |
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Sterol absorbtion inhibitors
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Exetimibe
Drops LDL 15% synergistic with statins Hepatotoxic? |
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Lipid lowering therapy choices
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1 statins
2 bile acid binding agents (first in pregnancy) 3 niacin, fibrates |
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Statins other therapeutic uses
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Anti inflammatory
Cancer prevention (colon) Neurodegenterative diseases (alzheimer's) |
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Classifications of CV disease
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Peripheral Vascular Disease:
Atherosclerotic Vasculitis Heart Disease: Coronary Artery Disease (CAD) Congenital Valve Disease Hypertensive Heart Disease Cardiomyopathy |
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Angina interventions
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ACE inhibitors
Beta blockers “Statin” ASA and/or clopidogrel (Plavix) ADP inhibitor |
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Stable angina treatment
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Nitrates
Beta Blockers Calcium Channel Blockers ACE inhibitors Hyperlidipemia treatment Esp. HMG-CoA Recuctase Inhibitors (“statins”) |
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isosorbide dinitrate
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Bidil Combo drug with nitro and Hydralazine
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Nitrate contraindications
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concurrent use with ED drugs ( -fils) sildenafil etc. viagra, levitra, cialis
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selective Beta 1 blocker
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Atenolol (tenormin)
Metoprolol (lopressor, Toprol) Effective in preventing attacks, reduce output and afterload |
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Nonselective beta blocke
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Propanolol (inderol)
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Cautions with B blockers
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negative inotrope, careful with dose.
Bradycardia, Av block, contraindicated for variant angina. |
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Ca Channel blocker
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Reduce Myocardial O2 demand, Prevent vasospasms, (eliminates variant angina in 70% of cases)
Prevents/ slows atheromatous plaques?... |
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CHF
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Ischemic
Non ischemic Idiopathic, post partum, cardiac toxins |
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CHF treatment strategy
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Digoxin (especially with A fib)
B Blockers in stable class II-IV CHF Vasodilators Treat hyperlipidemia Use statins? |
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CHF treatment strategy
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Digoxin (especially with A fib)
B Blockers in stable class II-IV CHF Vasodilators Treat hyperlipidemia Use statins? |
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CHF diuresis
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Spironolactone mya help prevent remodeling, prevent hypokalemia, Risky with ace inhibitors
Loop Diuretics, help in fluid overload, reduces Cardiac O2 demand, Reduces pre and afterload. some vasodilation effects |
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Chf Vasodilator
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Ice inhibitors or ARBS "mainstay"
Isosorbide +hydralazine (for african americans) Minoxidil |
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Amergent vasodilation
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Sodiium Nitroprusside
Nesiritide (from brain natriuretic peptide: Vasodialates, Diuretic) |
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CHF inotropes
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Cardiac Glycosides (DIG)
B agonists (Dobutamine, Dobutamide) Phosphodiesterase inhibitors (amrinone, Milrinone, Parenterals) |
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Cardiac Gllycosides
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Only oral inotrope,
INcrease intracellular Ca++, Increases cardiac Parasympathetic tone Low therapeutic index |
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Side effects of Digoxin
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Arrhythmias (heart block, conduction slowing, Irratible heart (PVC,VT,V fib)
Anorexia, nausea, HA, vision changes, fatique, estrogen effects |
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Factors for Dig toxicity
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Hypokalemia, Hypothyroidism, renal insufficiency
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Dig drug interactions
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Verapamil, corticosteroids, Quinidine, amiodarone
many more |
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Dig tox. tx
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Stop dig,
Treak K, neurtalize with Digibind, Digifab |
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When do you use Dig?
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As an adjunct,
In CHF with chronic a-fib |
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Anticoagulants for CHF
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Low dose ASA
In a-fib: Warfarin |
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CHF remodeling drugs
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Spironolactone,
ACE (lisinopril) and ARB (Losartan) Beta and Alpha blocker (carvedilol) |
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Causes of Impulse abnormalities
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Ischemia, hypoxia
PH problems: acidosis, alkalosis Excessive catecholamines Drug toxicity Overstretching of cardiac fibers Myocardial scar(s) |
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Genetic factors to abnormalities
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Polymorphic V tach (torsades)
Brugada syndrome (V fib) |
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Classes of antiarrythmics
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Class I
Na+ Channel Blockers Class II Beta Blockers Class III K+ Channel Blockers Class IV Ca++ Channel Blockers |
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Classes of antiarrythmics (specific drug examples)
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Class I:
Quinidine,Procainamide, Lidocaine Class II: Esmolol, Propanolol, Pindolol Class III: Sotalol, Amiodarone, Bretylium Class IV: Diltiazem, Verapamil |
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Drug of choice for V tach
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Lidocain, Amioderone
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Drug of choice for V fib
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Lidocain, amioderone, epinephrine
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Drug of choice for SVT
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Adenosine
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Drug of choice for A fib
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Propranolol, Amioderone
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A fib treatment
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Rate control
Beta blockers Digoxin Restore sinus rhythm Cardioversion Anticoagulation Warfarin (Coumadin) |
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Amiodarone effects
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Used to treat V tach and Fib, Atrial fib.
Can cause Pulmonary fibrosis, liver toxicity, Stops conversion of T4 to T3, Photodermatitis |
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inhibitors of CYP3A4
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Cimetadine( antacids)
Macrolides (erythromycin, clarithromycin) fluconazole Grapefruit juice Thus caution when taking these and amiodarone, rapid toxicity can deveolop |
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ICD or Amiodarone?
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ICD is primary tx, amio helps reduce ICD firing
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Digoxin uses
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A fib / flutter
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general classes of hormones
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Steroids, peptides, proteins, glycoproteins
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Example of cross sensitivity in hormone resceptors
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TSH in abundance in hypothyroidism can stimulate FSH receptors and produce ovarian cysts
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Major endocrine systems
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Adrenal
Thyroid Gonadal Growth Lactation Pancreatic Islets/Glucose Renin-Angiotensin-Aldosterone Others: Bone, Vasopressin |
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Anterior pituitary hormones
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ACTH
TSH FSH/LH Prolactin Somatotropin (Growth Hormone) |
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Hypothalamus hormones
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GnRH,
Vasopressin Oxytocin |
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Adverse effects of Growth Hormone
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hypothyroidism, Myalgia, arthralgia, CYP450 activation
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GH drugs
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Somatotropin, GH
GHRH Somatostatin, GH inhibiting hormone GH receptor antagonists |
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GH indications
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GH deficient,
Delayed growth Muscle augmentation in elderly? IUGR babies? |
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Somatostatin
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Octreotide, Lanreotide,
* used in acromegaly, carcinoid syndrom, Growth limitation, |
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prolactin
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Lactation, more.
Excess prolactin can cause galactorrhea, hypogonadism (low FSH and LH) excess from pituitary adenoma, primary hypothyroidism, or from drugs (dopamine blockers ie phenothiazine) |
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Hyperproalctinemia treatement
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Dopamine agonists
(ergot (a fungus)derived:)Bromocriptine (Parlodel) Pergolide (Permax) Cabergoline (Dostinex) Non ergot derived: parkinson agents or quinagolide outside USA) |
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Parkinsonian drug
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Dopamine agonsists
Bromocriptine (parlodel) |
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Gonadotropins
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Follicle stimulating hormone (FSH)
Luteinizing hormone (LH) Gonadotropin releasing hormone (GnRH) Human chorionic gonadotropin (HCG) |
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GnRH antagonist use and example
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Prevents premature ovulation
Controlled ovarian hyperstimulation (IVF) Cetrotide, Antagon |
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GnRH agonist use and example
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Down regulation (medical menipause, endometriosis, fibroids etc.
Lupron Zoladex Synarel |
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GnRH ise and example
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Infussion for hypothalamic amenorrhea (athletic or anorexic women)
Factrel, Lutrepulse |
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Gonadotropin use
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ovulation
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Gonadotropin sources
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Urine of women
Mentropins, HMG, Pergoal, Repronex, HCG Recombinant FSH or LH (fillistim, Gonal-F) |
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Posterior pituitary hormones and uses
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Oxytocin (pitocin, syntocinon) Augments labor milk letdown.
Vasopressin (ADH, Pitressin) Treats diabetes insipidis, Desmopressin (DDAVP, Stimate) |
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Parkinsonian drug
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Dopamine agonsists
Bromocriptine (parlodel) |
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Gonadotropins
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Follicle stimulating hormone (FSH)
Luteinizing hormone (LH) Gonadotropin releasing hormone (GnRH) Human chorionic gonadotropin (HCG) |
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GnRH antagonist use and example
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Prevents premature ovulation
Controlled ovarian hyperstimulation (IVF) Cetrotide, Antagon |
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GnRH agonist use and example
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Down regulation (medical menipause, endometriosis, fibroids etc.
Lupron Zoladex Synarel |
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GnRH ise and example
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Infussion for hypothalamic amenorrhea (athletic or anorexic women)
Factrel, Lutrepulse |
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Gonadotropin use
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ovulation
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Gonadotropin sources
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Urine of women
Mentropins, HMG, Pergoal, Repronex, HCG Recombinant FSH or LH (fillistim, Gonal-F) |
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Posterior pituitary hormones and uses
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Oxytocin (pitocin, syntocinon) Augments labor milk letdown.
Vasopressin (ADH, Pitressin) Treats diabetes insipidis, Desmopressin (DDAVP, Stimate) |
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thyroid production/
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Hypothalamus releases TRH (or TRF) which stimulates the qnterior pituitary to release TSH (and prolactin)
Inthyroid Tyrosine is iodinated to T3 or T4 TSH releases T3 and T4 from Thyroglobulin in thyroid follicles. T3 and T4 is transported via thryoxine binding globulin. (estrogen increase TBG androgens decrease TBG) T4 is converted peripherally to T3. T3 binds to nuclear receptor. |
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TRH (or TRF) use
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Testing Pituitary reserve of TSH or prolactin (usually just measure TSH,PRL.)
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Thyroid pathology
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Primary (gland failure)
Hashimoto low iodine intake, absence or destruction of gland Hyperthyroidism Graves disease Toxic nodular goiter (Plummer's disease) Neoplasms |
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T4 metabolism
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Liver CYP450
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Hyperthyroidism treatment
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B blockers,( for tachycardia, ischemia, tremors, agitation: Non-selective best ie propranolol, but caution with asthma CHF.)
Anti thyroid agents, (prevent thyroid storm) Destroy thyroid |
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Antithyroid agents
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Thioamides
Anion Inhibitors Iodides Iodinated contrast media Radioactive iodine |
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Thioamides MOA
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Blocks synthesis of T3/T4
-Propylthiouracil(PTU) q 6 best for pregnant -Methimazole qd. |
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Thioamine adverse effects
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Rash edema agranulocytosis
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Anion inhibitors
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Prevent reuptake of iodide
-Potassium perchlorate Can cause aplastic anemia Avoid if radioiodine use likely Thioamides first line of tx |
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Iodinated Contrast medium
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Block T4 to T3 conversion.
Iopanpoic acid (Telepaque) Diatrizoate sodium (Hypaque) Ipodate sodium (Oragrafin) |
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Thyrotoxic crisis
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Life threatening, pull out all the stops!
Beta blocker (propranolol) ,Ca+ channel blocker (diltiazem) Potassium iodide PTU (propylthiouracil Hydrocortisone (CV stability and reduced T4 to T3 conversion. |
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Immune system catagories
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Innate or Adaptive
each has cellular and humorsal components. Innate cellular: Macrophages, Granulocytes, Nk cells Adaptive Cellular: T and B lymphocytes Inate humoral:Complement Adaptive humoral: Immunoglobulins. |
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Antiinflamatory drugs
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NSAIDS
SAIDS (glucocorticoids: steroids) |
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Immmunosupressant drugs
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Glucocorticoids (“steroids”)
Cytokine Inhibitors Antimetabolites Monoclonal antibodies |
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Immunosupressive indications
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Allergy treatment
Autoimmune disease treatment(RA Lupus) Prevention of allograft rejection |
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Steroid classes with examples
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Estrogens
Estradiol Progestins Progesterone Glucocorticoids Cortisol Androgens Testosterone, Androstenedione, DHEA-S Mineralocorticoids Aldosterone |
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Glucocorticoid actions
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Glucose Production (Gluconeogenesis)
Resistance to Stress Glucose available Raise blood pressure Hematopoietic Lower lymphocyte/monocyte levels Anti-Inflammatory Lower lymphocyte levels Lower prostaglandin production Others Increase Gastric Acid, Pepsin Increase Bone Loss Muscle Weakness Mental Status Anti-emetic properties |
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Mineralocorticoid action
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Mineralocordicoid helps the body retain NA and H2O
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Glucocorticoid adverse effects
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Weight Gain (Central Obesity)
Impaired Healing Bone Loss/Osteoporosis Edema Peptic Ulcers Euphoria Hallucinations Adrenal Suppression* |
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Antiinflamatory: antimetabolites
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Azothioprine
Mycophenolate mofetil - organ transplants, RA -Oppertunistic infections a problem |
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Cytokines
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Protein hormone that modulate immune response
ie: TNF A IL 1-18 |
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Cytokine inhibitors
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Cyclosporine - organ transplants, RA. Nephrotoxic.
Tacrolimus (nephrotoxic, neurotoxic. Sirolimus (hyperlipidemia) |
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