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227 Cards in this Set
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What is the mech and side effects of
HYDRALAZINE? |
increases cGMP --> SM relaxation
vasodilates arteries >veins (decreased afterload) -tachycardia (contraindicated in angina/CAD), fluid retension, nausea, HA, angina. LUPUS LIKe snydrome |
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What is the mech and side effects of:
minoxidil |
K channel opener- hyperpolarizes SM cells in relaxed state
treatment of severe HTN -hypertrichosis, pericardial effusion, reflex tachy, angina, salt retention |
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what Ca channel blocker is contraindicated in arrythmias?
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Nifedepine
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Side effects of Calcium channel blockers
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Cardiac depression, peripheral edema, flushing, dizziness
CONSTIPATION |
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Name the mech of FENOLDOPAM.
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Dopamine D1 receptor agonist
relaxes vascular smooth muscle (think fenolDOPAMINE) |
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Name the mech of DIAZOXIDE.
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K channel opener- hyperpolarizes and relaxes vascular smooth muscle
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What is often given with nitrates for chest pain?
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B blockers-
prevent reflex increase in contractility and increase in heart rate |
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When do you use Ca channel blockers in CHF?
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patient has HTN and/or Angina
-DO NOT use verapamil/ diltizem(decreases ionotropy) give amlodipine/delodipine |
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What is the mech of Niacin?
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Inhibits lipolysis in adipose tissues
reduces hepatic VLDL secretion in circulation |
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What is colesevelam. name two drugs like it and contraindications
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Colesevelam, colestipol, and cholestyramine are bile acid binding resins
slightly increase HDL and Triglycerides, decrease LDL Contraindicated in gallstones and patients hat taking it due to GI discomfort |
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A patient taking anti lipid drugs comes in with osteoporosis. what drug?
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Bile Acid binding resins- Cholestyramine, colestipol, colesevelam
this is also contraindicated in women with gallstones |
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What does Ryanodine do?
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poison that inhibits Ca channel on Sarcoplasmic reticulum of Cardiac muscle
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what EKG changes are seen in Digoxin toxicity?
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Increase PR, decrease QT, scooping of ST segment, T Wave inversion on ECG
also causes increase parasymp activity (nausea, vomiting, diarrhea, blurry yellow vision) |
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What does quinidine due to digoxin clearance?
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decreases digoxin from tissue-binding sites
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Treatment for digoxin toxicity:
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normal K+ slowly, lidocaine, cardiac pacer
anti-dig Fab fragments, Mg2+ |
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What is the toxicity of quinidine?
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Cinchonism - HA, tinnitus
Thrombocytopenia Torsades de pointes (increase QT interval) -may cause digoxin toxicity |
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What is a toxicity of procainamide?
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SLE-like syndrome (Anti-histone Ab+)
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What is the treatment for digitalis induced arrhythmias?
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Class IB- lidocaine, Mexiletine, Tocainide
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What is the toxicity of Class IB antiarrhythmics?
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Cardiovascular depression, local anesthesia, CNS stimulation/ depression
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when are class IC antiarrhythmics contraindicated?
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Post MI
significantly prolongs the AV Node |
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what does metoprolol do to lipids?
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causes dyslipidemia
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Name the K channel blocking antiarrhythmics.
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Sotalol
Ibutilide Amiodarone, Dofetilide |
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What are the toxic effects of amiodarone?
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pulm. fibrosis, corneal deposits, HEPATOTOXIC, skin deposits (photoedermatitis), neuro defects, constipation, HYPOTHYROIDISM/ HYPERTHYROIDISM
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What drugs are used to prevent nodal arrythmias by primarily affecting the AV nodal cells?
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Ca channel blockers (Verapamil, diltiazem)
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What are the side effects of Ca channel blocking antiarrythmics?
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Constipation, flushing, edema, CHF, AV block, sinus node depression
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what is the drug of choice for diagnosing AV nodal arrhythmias?
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Adenosine
Increases K efflux--> hyperpolarizes cell and decreases I ca2+ |
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Treatment for nephrogenic diabetes insipidus (3)
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Amiloride (K sparring diuretic )
Indomethacin Hydrochlorothiazide diuretics |
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treatment for SIADH?
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Demecloycline or H20 restriction
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Drug causes of SIADH?
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Chlorpropamide, sulfonylurea
CYCLOPHOSPHAMIDE |
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Insulin treatment for acute DKA?
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Regular acting (peaks in 2-3 hours)
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When do Lispro and Aspart peak?
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Very short acting insulins peak at 30 minutes (tx of post meal hyperglycemia)
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What is Tolbutamide?
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First generation sulfonylurea
Mech: Closes K+ channels--> cell depolarizing and triggering INSULIN release via Calcium influx |
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What is the toxicity of Tolbutamide?
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1st gen sulfonylurea =
disulfiram like effects |
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What is Chlorpropamide?
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First generation sulfonylurea
Mech: Closes K+ channels--> cell depolarizing and triggering INSULIN release via Calcium influx |
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What is the toxicity of Chlorpropamide?
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1st gen sulfonylurea =
disulfiram like effects |
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What is Glimepiride? Name some similar drugs and give Mech and toxicity
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Glyburide and Glipizide = 2nd gen sulfonylureas
triggers insulin release via K+ channel closure and increase Ca influx toxicity: hypoglycemia, jaundice contraindicated in women trying to get pregnant |
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What are thiazolidenedones?
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Glitazone drugs (Pioglitazone / Rosiglitazone)
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How do glitazone drugs work?
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Increase target cell response to insulin via Adipokines (adiponectin) --> feeling of satiety
work via PPAR-gamma (a transcription factor) |
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What is the toxicity of glitazone drugs?
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Weight gain, edema, hepatotoxicity, CV Toxicity
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What is Miglitol?
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alpha-GLUCOSIDASE Inhibitor (along with acarbose)
toxicity= GI disturbance |
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What is pramlintide?
mech and toxicity? |
Decreases Glucagon
causes hypoglycemia, nausea, and diarrhea |
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What is Exenatide? Mech and toxicity?
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GLP-1 mimetic Increases insulin, decreases glucagon release
Increases feeling of satitety, decreases gastric emptying Toxicity: N/V/ Pancreatitis |
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What is Orlistat?
mech and toxicity? |
Mech: alters fat metabolism by inhibiting pancreatic lipase
"orlistat gets rid of fat" -used for tx of long-term obesity toxicity: steatorrhea, GI discomfort, reduced fat absorption of vitamins, HA |
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What is sibutramine?
mech, clinical use, and toxicity? |
Sympathomimetic Seratonin and Norepi reuptake inhibitor
used for short and long-term obesity management Causes Hypertension and tachycardia in toxicity |
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What drug has a 5' deiodinase in peripheral tissue?
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Propyltiouracil (decreases peripheral conversion of T4 to T3)
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What is the toxicity of PTU and methimazole?
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skin rash, agranulocytosis (rare), aplastic anemia
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What is an endocrine tx for Turner's syndrome?
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GH
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What is the clinical uses of Somatostatin (octreotide)?
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acromegaly, carcinoid, gastrinoma, glucagonoma
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What is triamcinolone?
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Glucocorticoid (along with hydrocortisone, prednisone, dexamethasone, beclomethasone)
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What is a toxicity of chronic triamcinolone tx?
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Glucocorticoid therapy--> Cushing syndrome
Peptic ULCERS DIABETES easy bruisability |
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What is the toxicity for Demeclocycline?
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ADH Antagonist (tetracycline family member)
causes photosensitivity, abnormalities of bone and teeth |
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What is Cabergoline?
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DA analogue (just like Bromocriptine)
can cause galactorrhea |
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What is famotidine? name some similar drugs.
Mech? |
H2 blocker- cimetidine, ranitidine, famotidine, nizatidine
Reversible block of H2 receptors--> decrease H+ secretion used for Peptic Ulcers, gastritis, mild esophageal reflux |
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Cimetidine toxicity.
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Inhibitor of P-450
Antiandrogenic effects (prolactin release, gynecomastia, impotence) Cross BBB (dizziness, confusion) |
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How do cimetidine and ranitidine affect renal function?
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decrease renal excretionof creatinine
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What is the treatment for Zollinger-Ellison?
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Lansoprazole, Omeprazole
irreversibly inhibit Na/K ATPase in parietal cells |
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What is the triple therapy for H. Pylori?
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Metronidazole, Amoxicillin (or Tetracycline), Bismuth
also use a PPI |
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Name the Drug: PGE1 analog
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Misoprostol
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What is the toxicity of misoprostol?
when is it contraindicated? |
Diarrhea
Contraindicated in childbearing age women (is an abortifacient) |
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What is Pirenzepine?
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Muscarininc antagonist used to block M1 receptors on ECL cells of the gut to DECREASE HISTAMINE secretion
also binds to M3 receptors on parietal cells (decrease H+ secretion) |
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What is propantheline?
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Muscarininc antagonist used to block M1 receptors on ECL cells of the gut to DECREASE HISTAMINE secretion
also binds to M3 receptors on parietal cells (decrease H+ secretion) |
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What is the symptoms associated with overusing:
Al OH |
constipation, hypophosphatemia
prox muscle weakness osteodystrophy seizures |
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What is the symptoms associated iwth overuse of MAGNESIUM HYDROXIDE?
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diarrhea, hyporeflexia, hypotension, cardiac arrest
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What is the clinical use of Infliximab and its mech?
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Crohn's disease, Rheumatoid arthritis
monoclonal Ab to TNF |
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What is a consequence of infliximab tx?
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respiratory infections (reactivation of TB), fever, hypotension
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What is sulfasalazine?
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combo of sulfapyridine (antibacterial) and mesalamine (anti-inflammatory)
used to tx of Crohns and Ulcerative colitis |
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What is the toxicity of sulfasalazine?
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malaise, nausea, sulfonamide toxicity, REVERSIBLE OLIGOSPERMIA
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What is an opiate treatment for acute cholecystitis and why do you use this particular one?
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Meperedine
does not cause vasospasm of sphincter of oddi (antimuscarinic) therefore preferred over other opiates |
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What is diphenoxylate?
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Mu opiate
Used to decrease motility |
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What is metoclopramide?
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D2 receptor antagonist
used to increase resting tone, contractility, LES tone, motility used for Diabetic and post-surgery gastroparesis! DOES NOT influence colon transport time |
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What is the toxicity of metoclopramide?
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(D2 receptor antagonist)
parkinsonian effects. restlessness, drowsiness, fatigue, depression, nausea, diarrhea |
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What drugs do metoclopramide interact with (2)?
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digoxin and diabetic agents
metoclopramide= D2 receptor antagonist |
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When is metoclopramide contraindicated?
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small bowel obstruction due to increase gastric motility
D2 receptor antagonist--increases resting tone, contractility, LES tone, motility used for diabetics and post surgery gastroparesis |
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What is prochlorperazine?
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DA antagonist used for tx of N/V
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What is scopalamine?
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Muscarinic antagonist used for tx of motion sickess, preop nausea
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What is aprepitant?
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NK1 antagonist (used for block NK1 receptor on medulla emetic reflex
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What are the toxicities of heparin?
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bleeding
THROMBOCYTOPENIA (HIT) Osteoporosis drug-drug interactions |
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What is enoxaparin?
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new LMW Heparin
acts more on Xa and with better bioavailability and 2-4x the half-life |
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What is heparin induced thrombocytopenia?
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heparin binds platelets and causes Ab production that DESTROYS PLATELETS and OVERACTIVATES remaining ones
thrombocytopenic & hypercoagulable state |
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What is hte mech of Lepirudin and Bivalirudin?
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Hirudin derivatives that DIRECTLY INHIBIT THROMBIN
used as an alternative in Heparin Induced thrombocytopenia |
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What is the respiratory and neurological toxicities of aspirin?
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Hyperventilation
Tinnitus (CN VIII) |
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What is the mech of clopidogrel and ticlopidine?
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inhibit platelet aggregation via IRREVERSIBLE BLOCK of ADP receptors (IIb/ IIIA)
also inhibits fibrinogen binding by preventing glycoprotein IIB/ IIIa expression |
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What is the toxicity of Ticlopidine?
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neutropenia
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What is abciximab?
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monclonal Ab to IIB/ III a receptors
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What is the toxicity of abciximab?
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bleeding, thrombocytopenia
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How does methotrexate work?
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Folate acid analog that inihibits dihydrofolate reductase (preventing formation of dTMP)
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What is the indications for methotrexate use?
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leukemias, lymphomas, choriocarcinoma, sarcomas
Abortion, ectopic pregnancy Rheumatoid arthritis, psoriasis |
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What is the histological change seen in the liver with methotrexate use?
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macrovesicular fatty change
hepatotoxic |
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What is the hematological side effect of methotrexate use and how is it treated?
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myelosuppresion
treated with leucovorin (folinic acid) |
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What is the mucosal toxicity of methotrexate use?
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stomatitis, mucositis
(mouth ulcers) |
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What is apprepitant?
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NK1 antagonist (on anti-emetic center of medulla)
tx for chemo induced N/V |
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What is 5-Fluorouracil?
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prymidine analog that is bioactivated to 5F-dUMP
used for Colon cancer |
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what is 5-fluorouracil toxicity and its treatment?
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Myelosuppresion
NOT treatable with leucoverin (methotrexate is) Tx of toxicity = THYMIDINE also causes photosensitivity |
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What increases 6-mercaptopurine toxicity?
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Allopurinol (mercaptopurine metabolized by xanthine oxidase)
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What activates 6-mercaptopurine?
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HGPRTase
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what is the mech and toxicity of ctyarabine?
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inhibits DNA polymerase
leukopenia, thrombocytopenia, megaloblastic anemia |
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What is the mech for cyclophosphamide/ ifosfamide?
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alkylating agents
covalently cross-link (interstrand) DNA at guanine N-7 requires bioactivation by liver! used in Treatment of Wegner's, PAN this drug can cause SIADH |
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What is the toxicity of cyclophosphamide?
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myelosuppression, hemorrhagic cystitis (prevent with mesna)
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What are the nitrosoureas and what is their mech?
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Carmustine, lomustine, semustine, STREPTOZOCIN
DNA alkylators that need to be BIOACTIVATED these cross BBB (brain tumors) |
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What is the toxicity of Streptozocin?
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Nitrosoureas (carmustine, lomustine, semustine, streptozocin)
all can cross BBB--> CNS Toxicity (dizziness/ataxia) |
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What is the toxicity of cisplatin/ Carboplatin?
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Cisplatin/Carboplatin = DNA cross-linkers
NEPHROTOXIC, acoustic nerve damage |
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What is the mech of Busulfan?
Toxicity? |
Alkylates DNA
causes PULMONARY FIBROSIS and HYPERPIGMENTATION |
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What is the mech of adriamycin?
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Doxorubicin / Daunorubicin
generate free radicals and non-covalently intercalate in DNA (creates breaks in DNA strand to decrease replication) |
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What is the non-cardio toxicities of Doxorubicin and daunorubicin?
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MYELOSUPPRESION and MARKED ALOPECIA
toxic extravasation |
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What is the mech for Dactinomycin/ actinomycin?
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Intercalates DNA
childhood tumors- wilm's tumor, Ewing sarcoma, Rhabdomyosarcoma |
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What is the toxicity for Dactinomycin?
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myelosuppresion
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What is a prominent minimal side effect of bleomycin?
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Bleomycin (causes free radical damage--> DNA strand breaks)
(toxicity= pulm. fibrosis, skin changes) MINIMAL MYELOSUPPRESSION |
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what is the mech for Hydroxyurea?
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inibits ribonucleotide reductase--> Decreased DNA synthesis
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What is the toxicity of Hydroxyurea?
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bone marrow suppression, GI upset
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What is the carcinoma associated with Tamoxifen use?
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Endometrial Cancer (has partial Estrogen agonist effects--> hot flashes)
this is not seen in Raloxifene (endometrial antagonist) |
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What is the mech of Trastuzumab?
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monoclonal Ab against Her-2 (erb-B2)
helps kill breast cancer cells that ocerexpres HER-2 toxicity: cardiotoxicity |
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What is the toxicity of trastuzumab?
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Cardiotoxicity
(monoclonal Ab to ERB-B2 in breast cancers...may cause Ab mediated toxicity) |
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What is a side effect of imatinib (gleevec)
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used to inhibit CML bcr-abl tyrosine kinase
causes FLUID RETENTION |
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what does vincristine and vinblastine do?
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inhibit polymerization of microtubules--> no mitotic spindle formation
vincristine= neurotoxicity (areflexia, peripheral neuritis), paralytic ileus Vinblastine- BLASTS bone marrow |
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What is the toxicity of Vincristine and Vinblastine?
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Vincristine- neurotoxic (peripheral neuritis, areflexia), Paralytic ileus
VINBLASTINE- BLASTS the bone marrow |
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What is the toxicity of paclitaxel?
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myelosuppression and hypersensitivity
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Cephalosporin treatment for Pseudomonas?
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Ceftazidime (3rd generation)
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4th generation cephalosporin for Pseudomonas?
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Cefepime
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What do cephalosporins cross react with in toxicity?
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Aminoglycosides to cause nephrotoxicity
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What happens if you take a cephalosporin and drink alcohol?
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Disulfiram like reaction with ethanol (seen in Cefamandole)
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What is the mech of Aztreonam?
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inhibits cell wall synthesis (binds to PBP3) - KILLS ONLY GRAM - RODS (klebsiella, pseudomonas, serratia)
synergistic with aminoglycosides |
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What is special about the toxicity of Atreonam
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NO Cross sensitivity with Penicillin (GIVEN TO PATIENTS WITH PENICILLIN ALLERGY)
(Penicillianase resistant Ab, binds to PBP3, used for GRAM - RODS ONLY) |
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What are the toxicities of Imipenam?
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Impipenam (always given with cilistatin to inhibit renal dihydropeptidase I)
causes GI distress, skin rash, CNS TOXICITY (seizures) |
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Vancomycin toxicity:
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NOT:
Nephrotoxic Ototoxic Thrombophlebitis "red man syndrome"- diffuse flushing (pretreat with antihistamines + slow infusion rate) |
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What do aminoglycosides prevent?
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A-site tRNA binding
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What is required for Aminoglycosides to become active?
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needs O2 for uptake (ineffective against anaerobes)
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What is the toxicity of aminoglycosides?
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Nephrotoxic
Ototoxic (VIII--> hearing loss, vertigo) Teratogen |
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What other type of drugs increase the ototoxicity of amingoglycosides?
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Loop diuretics increase the otoxocity of amingoglycosides
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How is doxycycline eliminated?
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renally excreted. CANNOT BE USED in patients with renal failure
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What are the organisms susceptible to tetracyclines?
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VACUUM THe BedRoom
V. Cholera Acne Chlamydia Ureaplasma Urealyticum Mycoplasma pneumo Tularemia (francisella) H. Pylori Borrelia Rickettsia |
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What is the toxicity of Macrolides?
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GI Discomfort = most common cause of non-compliance
Acute cholestatic hepatitis eosinophiluria skin rashes |
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What do marcolides due to theophyllines / oral anticoagulants?
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macrolides increase concentration of oral anticoagulants and theophyllines
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Newborn with abd. distension, pallid cyanosis, vasomotor collapse, irreg. respiration, refusal to suck, loose, green stools. WHAT DRUG?
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Chloramphenicol "Gray baby"
due to lack of liver UDP-glucuronyl transferase |
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What is a toxicity infection of clindamycin?
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pseudomembranous colitis
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What enzyme is inhibited by trimethoprim/pyrimethaine?
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Dihydrofolate reducatase
(can't make tetrahyrofolic acid) |
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What enzyme is inhibited by sulfonamides?
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Dihydropteroate synthetase
(can't make dihydropteroic acid) |
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what is the toxicity of sulfonamides?
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hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity (tubulointerstitial nephritis)
photosensitivity, kernicterus (infants) |
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What does sulfonamides do to albumin?
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displaces albumin binding drugs (warfarin)
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What is the mech of Trimethoprim?
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inhibits bacterial dihydrofolate reductase
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what is the toxicity of trimethoprim?
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MEGALOBLASTIC ANEMIA, leukocytopenia, granulocytopenia
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What leukotriene does colchicine inhibit?
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Leukotriene B4
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What does PGI2 do?
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Decrease platelet aggregation
decrease uterine tone |
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What does PGE2 do? 4 things
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Decrease vascular tone
Increase Pain Increase uterine tone Increase Temperature |
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At whose doses does aspirin have to be an anti-inflammatory?
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2400-4000 mg/day
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At what doeses does aspirin have to be to be antipyretic and analgesic?
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200-2400 md/day
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What is the toxicity of aspirin?
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Gastric upset
ACUTE RENAL FAILURE INTERSTITIAL NEPHRITIS Upper GI bleeds |
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what is naproxen?
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NSAID
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what nsaid is used to close a PDA?
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indomethacin
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What is the toxicity of NSAIDS?
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Renal damage
Aplastic anemia GI distress Ulcers |
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What allergies are seen with Cox-2 drugs?
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Sulfa allergies ( seen with celecoxib, furosemide, probenicid, TMP-SMX, sulfasalazine, sulfonylurea, sumatriptan)
FEVER, rash, STEVEN JOHNSON SYNDROME, Hemolytic anemia, thrombocytopenia, urticaria, hives, agranulocytosis |
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Where does Acetaminophen primarily work in the body?
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mostly in CNS, reversibly inhibits cyclooxygenase (lacks anti-inflammatory properties)
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what is the Toxicity of Acetaminophen?
|
hepatic necrosis (decrease glutathione) tx- N acetylcysteine
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What is the mech for Pamidronate?
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Inhibit osteoclast activity
Reduces both formation and resoprtion of hydroxyapatite |
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What is the GI toxicity of Pamidronate?
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Bisphosphonate (inhibits osteoclasts)
corrosive esophagitis, nausea, diarrhea |
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What is the mech of Colchicine?
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Used in Acute gout attacks
stabilizes tubulin and inhibits microtubule polymerization impairs leukocyte chemotaxis and degranulation |
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Where do you see the side effects of Colchicine?
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(impairs leukocyte chemotaxis/degranulation 2. stabilizes tubulin and inhibits microtubule polymerization)
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What is Probenecids mech?
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inhibits reabsorption of uric acid in PCT
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What is probenecides effect on Penicillin?
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Probenecid (inhibits uric acid reabsorpt in PT)
INHIBITS penicillin reabsorption in the PT |
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What drugs decrease the secretion of uric acid in the PT?
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Diuretics and low-dose salicylates
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What is Etanercept and when is it used (3 diseases)
|
Remcombinant form of TNF receptor that binds TNF
used in RA, psoriasis, ankylosing spondylitis |
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What is infliximab and when is it used?
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Anti-TNF antibody
used in Crohn's disease, RA, and ankylosing spondylitis |
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What is the mech of cyclobenzaprine?
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skeletal muscle relaxant - Tricyclic acting
works at brain stem |
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What is the side effect of Gold Salts?
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used to treat severe RA (decreases lysosomal and mass fx)
side effects: dermatitis, hematotoxicity, nephrotoxicity |
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When are opiods contraindicated?
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Head injury due to increases intracranial pressure
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What is the mech and use of Methysergide?
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prevention of migraine HA (blocks 5-HT receptors)
Can be used for carcinoid tumors |
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What is a toxicity of methysergide?
|
(5HT receptor blocker used for prevention of migraine/carcinoid syndrome)
RETROPERITONEAL/ SUBENDOCARDIAL FIBROPLASIA |
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What is the use of thalidomide?
|
potent immunosuppressant (used in Tx of SLE, mult. myeloma, leprosy)
Decreases TNF-Alpha |
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What is the mech of Epinephrine use in glaucoma? what is the contraindication?
|
Used in open angle glaucoma--causes vasoconstriction
do not use in closed angle-glaucoma |
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What B blockers are used to treat Glaucoma? (3)
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Timolol, Betaxol, Carteolol
they decrease aqeous humor synthesis no pupillary of vision changes |
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How does Azatazolamide work in glaucoma?
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decreases aqeuos humor snythesis due to decreasing HCO3
no pupillary or vision changes |
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What cholimemetics are used to treat Glaucoma? (4)
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Pilocarpine, carbachol, physostigmine, echothiophate
-increases outflow of aqeuous humor, contract ciliary muscle and open trabecular meshwork PILOCARPINE in emergencies all very effective at opening Canal of Schlemm |
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What is the side effect of Echothiophate for glaucoma?
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Cholimemetic: Pilocarpine, carbachol, physostigmine, echothiophate
-increases outflow of aqeuous humor, contract ciliary muscle and open trabecular meshwork SIDE EFFECTS: MIOSIS, CYCLOSPASM |
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What is the side effect of Latanoprost for glaucoma treatment?
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(increases outflow of aqueous humor)
DARKENS COLOR OF IRIS (browning) |
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What is the mech of Dextromethorphan?
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OPIOD Analgesis (works at opiod receptos (mu= morphine delta = enkephalin kappa = dynorphin) to MODULATE SYNAPTIC TRANSMISSION
OPENS K channels, closes CA channels --> decreases synaptic transmission |
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What is the use of dextromethorphan?
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opiod analgesic
used for Cough suppression |
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What ist he use of diphenoxylate?
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Opiod analgesis OPIOD Analgesis (works at opiod receptos (mu= morphine delta = enkephalin kappa = dynorphin) to MODULATE SYNAPTIC TRANSMISSION
OPENS K channels, closes CA channels --> decreases synaptic transmission USED FOR DIARRHEA |
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What does opiod analgesics due to the lung?
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morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan, diphenoxylate
TREATMENT FOR ACUTE PULMONARY EDEMA |
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What is the toxicity of opiod analgesics?
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Toxicity= respiratory depression, PINPOINT PUPILS, CNS DEPRESSION with other drugs
NO TOLERANCE TO MIOSIS and CONSTIPATION morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan, diphenoxylate OPIOD Analgesis (works at opiod receptos (mu= morphine delta = enkephalin kappa = dynorphin) to MODULATE SYNAPTIC TRANSMISSION OPENS K channels, closes CA channels --> decreases synaptic transmission |
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How is opiod toxicity treated?
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Naloxone / Naltrexone
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What is the mech of Butorphanol?
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Partial agonist at opiod mu receptors (agonist at KAPPA receptors)
Used for PAIN TX (less respiratory depression than full agonists) CAN CAUSE WITHDRAWAL if on full agonist |
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What is the mech, use, and toxicity of TRAMADOL?
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very weak opiod agonist, Inhibits seratonin and NE reuptake
used for Chronic pain Toxicity= respiratory depression, PINPOINT PUPILS, CNS DEPRESSION with other drugs NO TOLERANCE TO MIOSIS and CONSTIPATION **DECREASES SEIZURE THRESHOLD** |
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What is the mech of pentazocine?
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partial agonist at Mu receptor
can cause withdrawal symptoms (if pt on morphine) |
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What is the toxicity phenytoin?
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nystagmus, diplopia, ataxia, sedation, GINGIVAL HYPERPLASIA, HIRSUTISM, MEGALOBLASTIC ANEMIA, teratogenesis, SLE, Induces CTY. P450
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What is the mech of Phenytoin?
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Blocks NA channels (inhibits release of GLUTAMATE friom pre-excitatory neurons)
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What is the use of phenytoin?
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tonic-clonic seizures, Class IB antiarrhythmic
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What is thiopental used for?
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induction of anesthesia
barbiturate that causes I duration of Chloride channel opening (decreases neuron firing, assists GABA) |
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Toxicity of Barbiturates
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CNS depression with alcohol, dependence
RESPIRATORY/ CARDIOVASCULAR depression INCREASE CYT. -p450 CONTRAINDICATED IN PORPHYRIA |
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What is chlorodiazepoxide?
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Benzodiazepine (diazepam, larazepam, triazolom, temazepam, oxazepam, midazolam, alprazolam)
help GABA action by increases freq of Cl channel opening |
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What are 4 short acting benzodiazepines?
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Alprazolam
Triazolam Oxazepam, Midazolam HIGH ADDICTIVE POTENTIAL |
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What is the toxicity of Benzodiazepines?
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Dependence, CNS DEPRESSION with ALCOHOL
tx OD with flumazenil (comp. antagonist at GABA receptor) |
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What is the anesthetic principle behind a drug with decreased solubility in blood?
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rapid induction and recovery times
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What is the anesthetic principle in a drug with increases solubility in lipids?
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Increased potency (potency = 1/ MAC)
MAC decreases with age |
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What is the induction time and potency of N20?
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Low blood solubility= fast induction
Low lipid solubility = less potent |
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What is the induction and potency profile for Halothane?
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Increase lipid solubility= very potent
increase blood solubility = slow induction |
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What is the effect of a high AV gradient in an anesthetic?
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indicates increased tissue uptake
low onset of action as more gas needed to saturate tissues |
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What are some of the inhaled anesthetics?
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Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
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What is the effect of Enflurane?
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inhaled anesthetic: Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
MYOCARDIAL DEPRESSION, RESPIRATORY DEPRESSION, nausea/emesis, INCREASED CEREBRAL BLOOD FLOWQ (decrease cerebral metabolic demand) |
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What is the toxicity of halothane?
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hepatotoxic
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What is the toxicity of methoxyflurane?
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nephrotoxic
inhaled anesthetic: MYOCARDIAL DEPRESSION, RESPIRATORY DEPRESSION, nausea/emesis, INCREASED CEREBRAL BLOOD FLOWQ (decrease cerebral metabolic demand) |
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What is the toxicity of enflurane?
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PROCONVULSANT
inhaled anesthetic: MYOCARDIAL DEPRESSION, RESPIRATORY DEPRESSION, nausea/emesis, INCREASED CEREBRAL BLOOD FLOWQ (decrease cerebral metabolic demand) |
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What causes malignant hyperthermia?
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Inhaled anesthetics
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What is a toxicity of nitrous oxide?
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trapped gas
inhaled anesthetic: MYOCARDIAL DEPRESSION, RESPIRATORY DEPRESSION, nausea/emesis, INCREASED CEREBRAL BLOOD FLOWQ (decrease cerebral metabolic demand) |
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What is thiopental used for?
potency/ induction? |
Barbiturate- IV ANESTHETIC
High potency (increase lipid solubility) rapid induction (low blood solubility) used for INDUCTION and SHORT sx procedures DECREASES CEREBRAL BLOOD FLOW (as opposed to inhaled anesthetics that increase cerebral blood flow) |
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What is the use of Midazolam?
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Benzo - used for IV anesthetic
most common drug for Endoscopy -used with gaseous anesthetics and narcotics -may cause post-op respiratory depression, decrease in BP (treat OD with flumazenil) Causes AMNESIA |
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What is the indication for Arylcyclohexylamines (ketamine)
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PCP analog that acts as DISSOCIATIVE anesthetic
blocks NMDA receptor CARDIOVASCULAR STIMULANT causes disorientation, hallucination, bad dreams INCREASES CEREBRAL BLOOD FLOW |
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What is the propofol?
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IV anesthetic for rapid anesthesia induction, short procedures
LESS POST-OP nausea than THIOPENTAL potentiates GABA |
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What are the local anesthetic ESTERS?
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ESTERS- Procaine, cocaine, tetracaine
BLock Na channels by biding to part of channel (prefers activated Na channels-->better for rapidly firing neurons) |
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What are the amide anesthetics?
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Lidocaine, mepivacine, bupivacaine
BLock Na channels by biding to part of channel (prefers activated Na channels-->better for rapidly firing neurons) |
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how do you change anesthetic principles in infected tissues?
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infected= acidic tissues
alkaline anesthetics are charged so cannot penetrate as effectively INCREASE ANESTHETIC dose |
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What is the order of nerve blockage in fibers?
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small diameter > large diameter
Myelinated fibers > unmyelinated fibers small myelinated > small unmyelinated > large myelinated > large unmyelinated |
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What is the oder of loss for sensation in anesthetics?
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1. Pain
2. temp 3. touch 4. pressure |
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What is the toxicity of Bupivacaine?
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SEVERE CARDIOVASCULAR TOXICITY (\
(Amide anesthetic that blocks Na channels in active neurons) |
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What is a complication of succinylcholine?
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used for muscle paralysis in surgery/mechanical ventilation (selects motor nicotinic receptor)
HYPERCALCEMIA, HYPERKALEMIA |
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What is phase I and II depolarization in succhinylcholine?
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PHASE I- prolonged depolarization - no antidote. Block potentiated by cholinesterase inhibitors
Phase II - repolarized but still blocked antidote = cholintesteraes inhibitors (neostigmine) |
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What is a non-depolarizing neuromuscular blocker?
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tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
COMPETES WITH ACh for receptors reverse blockade- neostigmine, edrophonium, other cholinesterase inhibitors |
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What two drugs cause malignant hyperthermia?
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inhaled anesthetics (end in -ane) and succinylcholine
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What is the mech and use of bromocriptine?
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agonize dopamine Receptors (ergot
alkaloid with partial DA agonist properties) used in parkinsons |
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What is the mech of PRAMIPEXOLE?
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agonize dopamine Receptors in parkinsons dz
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What ist he mech of ropinirole?
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Agonist at DA receptors
used in Parkinsons |
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What does Amantadine do in Parkinsons?
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Amantadine- increases DA release
used as an antiviral (influenza A /rubella) TOXICITY= ATAXIA |
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What is the mech of seligiline?
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selectively inhibits MAO-B--> increase DA availability
may use as adjunt to L-DOPA toxicity: dyskinesia, akinesia between doses |
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What is the mech of Entacapone/ Tolcapone?
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COMT inhibitors
prevent dopamine breakdown |
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What is the Mech of Benzotropine?
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Benzotropine- antimuscarinic)
IMPROVES TREMOR and RIGIDITY no effect on bradykinesia |
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What are the toxicity of Levodopa, Carbidopa?
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peripheral conversion--> arrhythmias (prevented by carbidopa)
long term use-->dyskinesia, akinesia between doses levodopa-->confusion, hallucination, nightmares |
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What is the toxicity of Sumatriptan?
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Seratonin 1b/1D agonist --causes vasoconstriction, inhibition of trigeminal activation, and vasoactive peptide release.
CORONARY VASOSPASM (contraindicated in CAD, PRINZMETAL ANGINA), mild tingling |
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What is Memantine used for ? mech and toxicity?
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NMDA receptor antagonist
helps prevent excitoxicity mediated by Calcium DIZZINESS, CONFUSION, HALLUCINATIONS |
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What is the Donepezil?
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Acetylcholinesterase inhibitor
NAUSEA, Dizziness, INSOMNIA |
