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PhArmacology 101 > Exam 3 > Flashcards

Exam 3 Flashcards

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1
Q

Anticoagulant

A
  1. MOA: disrupt coagulation cascade = no fibrin produced
  2. # 1 = inhibit synthesis of clotting factors
  3. # 2 = inhibit the activity of clotting factors
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2
Q

Antiplatelet

A

Inhibit platelet aggregation

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3
Q

Thrombolytic

A

Promote lysis of fibrin = dissolution of thrombi

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4
Q

Unfractionated heparin

A
  1. Type: Rapid-acting anticoag
  2. MOA: enhances anti-thrombin
  3. Source: Lungs of cattle/intestine of pig
  4. Dose: INJECTION ONLY (IV or sub Q)
  5. Indications: Pregnancy anticoag, rapid coag required
  6. Therapeutic Use:
    1. PE,
    2. CVA (evolving),
    3. DVT,
    4. Open heart surgery,
    5. Renal dialysis,
    6. Low-dose therapy post op,
    7. Disseminated intravascular coag,
    8. Addition to thrombolytic
  7. Contraindicated:
    1. Thrombocytopenia,
    2. Uncontrollable bleeding,
    3. Post op - eye, brain, spine
  8. ADVERSE: Hemorrhage, HI thrombocytopenia, Hypersensitivity
  9. ANTIDOTE: Protamine Sulfate
  10. TESTS: aPTT
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5
Q

LMW Heparin

A
  1. Composition: shorter molecules than unfract.
  2. Therapeutic Use:
    1. Prevent DVT post surgery (including hip, knee),
    2. Treat DVT,
    3. Prevent Ischemic complications - (unstable angina, non-Q-wave MI, STEMI)
  3. Dose: SubQ - based on body weight
  4. ANTIDOTE: Protamine sulfate
  5. Pro/Con: $$$ more, no monitoring - give at home
  6. ADVERSE:
    1. Bleeding (less than Unfract.),
    2. Immune mediated thrombocytopenia,
    3. neurologic injury with spinal puncture or spinal epidural anesthesia
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6
Q

Enoxaparin

A

LMW Heparin

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7
Q

Dalteparin

A

LMW Heparin

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8
Q

Tinzaparin

A

LMW Heparin

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9
Q

Warfarin

A
  1. Type: anticoagulent (DELAYED ONSET)
  2. Dose: ORAL
  3. MOA: Blocks biosynthesis factors 7, 9, 10 and prothrombin, Vitamin K antagonists
  4. USE:
    1. Long term prophylaxis of thrombosis,
    2. prevent DVT and PE,
    3. Prevent Thromboembolism (pts with prosthetic heart valves,
    4. Prevent thrombosis during Afib
  5. ADVERSE:
    1. Hemorrhage,
    2. Vitamin K toxicity,
    3. fetal harm
  6. Contraindications:
    1. Emergencies,
    2. NO pregnancy
  7. DVD:
    1. increase anticoag,
    2. promote bleed,
    3. decrease anticoag,
    4. Heparin,
    5. Aspirin,
    6. Acetaminophen
  8. TEST: PT, INR (1-3 months to get stable)
  9. Facts: cows eating rotten clover - discovery, used as rat poison, failed suicide attempt with large dose peaked clinical interest
  10. ANTIDOTE: vitamin K
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10
Q

Aspirin

A
  1. Type: Antiplatelet
  2. MOA: inhib COXnase
  3. Adverse:
    1. GI bleed,
    2. hemorrhagic stroke,
    3. EC tabs may not reduce risk of GI bleed
  4. USE:
    1. Ischemic stroke,
    2. TIA,
    3. Chronic stable angina,
    4. unstable angina,
    5. coronary stenting,
    6. Acute MI,
    7. Previous MI,
    8. Prevent MI
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11
Q

Ticlopidine

A
  1. Type: Antiplatelet
  2. MOA: inhibits ADP-mediated aggregation
  3. ADVERSE: Hematologic effects
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12
Q

Clopidogrel

A
  1. Type: Antiplatelet
  2. MOA: ADP receptor antag (Blocks P2y12 ADP receptors on platelet surface = no ADP stim. aggregation)
  3. USE:
    1. Prevent coronary artery stent blockage,
    2. Reduce thrombotic events in pts with acute coronary syndrome,
    3. Secondary prevention of MI, Stroke, etc
  4. ADVERSE - see aspirin
  5. DVD: watch out for other bleeders
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13
Q

ABCiximab

A
  1. Type: Antiplatelet (GP IIb/IIIa receptor antag)
  2. MOA: reversible blockade of platelet receptors “SUPER ASPIRIN” (prevents platelets near GP IIb/IIIa from binding fibrinogen)
  3. Dose; effects linger for 23-48 hours
  4. Use: Acute coronary syndrome, percutaneous coronary interventions,
  5. DVD: OKAY with aspirin and heparin,
  6. USE:
    1. Iv therapy of ACS,
    2. PCI,
    3. Increase revascularization in pts with acute MI and thrombolytic therapy
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14
Q

Eptifibatide

A
  1. Type: Antiplatelet (GP IIa/IIIb inhibitor)
  2. MOA: reversible and highly selective
  3. USE: ACS, PCI
  4. Dose: effects reverse in 4 hours
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15
Q

Tirofiban

A
  1. Type: Antiplatelet (GP IIA/IIIB inhib)
  2. USE: reduce ischemic events with ACS and PCI
  3. DOSE: effects reverse in 4 hours
  4. ADVERSE: bleed
  5. DVD: NOT with drugs that suppress hemostasis
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16
Q

Dipyridamole

A

Antiplatelet with aspirin too

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17
Q

Cilostazol

A

Antiplatelet

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18
Q

Alteplase

A
  1. MOA: binds with plasminogen to for an active complex - complex catalyzing conversion of plasminogen to plasmin = enzyme that digests fibrin clots
  2. USE: MI, Ischemic stroke, PE (big)
  3. ADVERSE: Bleeding (ICP risk higher than with streptokinase), keep whole blood products around, Fever
  4. ANTIDOTE: Aminocaproic Acid
  5. Pro/Cons: No hypersensitivity, no hypotension
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19
Q

Tenecteplase

A
  1. Type: Thrombolytic
  2. Use: ONLY ACUTE MI
  3. Source: Human tissue plasminogen activator
  4. Pro/Con: ease of use
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20
Q

Reteplase

A
  1. Type: Thrombolytic
  2. Source: tPA produced by recombinant DNA
  3. Dose: Short half life (13-16 minutes)
  4. USE: ONLY ACUTE MI
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21
Q

Diabetes Mellitus

A
  1. Issue: Disorder of carbohydrate metabolism
  2. Type I: no insulin
  3. Type II: receptors resistant to insulin
  4. INSULIN: allows glucose to enter cells, w/o bg levels rise = hypergly, polyuria, polydipsia, ketonuria and weight loss *type important
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22
Q

T1DM

A
  1. Onset: childhood/adolescence 5% of cases
  2. Issue: destruction of pancreatic beta cells due to autoimmune process = no insulin
  3. Trigger: genetic, environmental, infectious, unknown
  4. Complications (short term): Hyperglycemia (disease), hypoglycemia (tx), Ketoacidosis
  5. Complications (long term):
    1. Macrovascular damage - injury to bv = many things (altered lipid metab),
    2. Microvascular damage = retinopathy, nephropathy, sensory/motor neuropathy, gastroparesis, amputation, ED
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23
Q

T2DM

A
  1. Onset: any time 90-95% of all cases 22 million americans
  2. Issue: Insulin resistance and impaired insulin secretion HYPERINULINEMIA hereditary
  3. Complications (short term): Hyperglycemia (disease), Hypoglycemia (tx), Hyperosmolarity (Of blood with extreme hyperglycemia)
  4. Complications (long term):
    1. Macrovascular damage- injury to bv = many things (altered lipid metab),
    2. Microvascular damage = retinopathy, nephropathy, sensory/motor neuropathy, gastroparesis, amputation, ED
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24
Q

Diagnosing DM

A
  1. Hemoglobin A1C = % of glycosylated hemoglobin (found in blood attached to a glucose molecule) = average for last 2-3 months)
  2. Fasting Plasma Glucose
  3. Casual plasma glucose (non-fasted)
  4. Oral glucose tolerance test (pre/post high sugar drink)
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25
Q

Pre diabetes

A

impaired fasting glucose - 100-125 many people never develop

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26
Q

Tx DM

A
  1. diet - depends on person, low glycemic
  2. Physical activity Insulin replacement
  3. Manage HTN - ACE (lisinopril) or ARB (losartan)
  4. lower kidney risk
  5. Tx Dyslipidemia - Statins (atorvastatin)
  6. Screen and treat for HTN nephropathy, retinopathy, neuropathy, dyslipidemia
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27
Q

Glucose target

A
  1. Pre meal: 70-130
  2. Post meal: 100-140
  3. A1C test: usual human = 7% but DM human = 8% to avoid hypoglycemic attack
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28
Q

Insulin

A
  1. Made in pancreas
  2. Released by pancreas
  3. Moves glucose into cells
  4. Promotes glycogen formation
  5. w/o =
    1. Break down glycogen,
    2. increased glycogenolysis ,
    3. increased gluconeogenesis,
    4. reduced glucose utilization
  6. HIGH ALERT MEDICATION
  7. Source = bovine, porcine, human
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29
Q

Insulin ASPART

A
  1. Rapid onset (10-20 mins0
  2. Short duration (3-5 hours)
  3. Analog of Human Insulin
  4. Note: dose immediately before or after eating
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30
Q

Insulin LISPRO

A
  1. Rapid acting (15-30 mins)
  2. Duration: 3-6 hours
  3. Dose SUBQ or pump 5-10 minutes before meals
  4. Faster than R but shorter
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31
Q

Insulin GLULISINE

A
  1. Rapid onset (10-15mins)
  2. Short duration (3-5hours)
  3. Synthetic analog of human
  4. Dose: near time of eating
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32
Q

Regular insulin

A
  1. Moderate action: (30-60 mins)
  2. Peak - 1-5 hours
  3. Duration - 10 hours
  4. Dose: SubQ, SubQ infusion, IM (rare) and oral inhalation (not currently used)
  5. U100 or U500 vials
  6. Note: unmodified human insulin
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33
Q

NPH insulin

A
  1. Dose: give 2 or 3 times daily (between meals and overnight)
  2. SubQ injection only
  3. CAN MIX WITH SHORTER ACTING
  4. Adverse: Hypersensitivity is possible
  5. CLOUDY MUST AGITATE
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34
Q

Insulin GLARGINE

A

Duration: 24 hours

Dose: 1x daily T1 (kids and adult) T2 (adult)

SubQ

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35
Q

Dosing schedule of Insulin

A
    • Twice daily premixed
    • Intensive basal/bolus strategy
    • continous subcutaneous insulin
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36
Q

Complications of Insulin

A
  1. Hypoglycemia - BG < 70 -
  2. repeated = Adrenergic response - jittery, tachy, sweating, dizzy, hungry -
  3. worse - LOC change, mental status change, confusion, words slurred, coma
  4. With frequent episodes- cut right to coma b/c overstimulation of receptors
  5. Must control BG tightly
  6. Tx= Sugar, Iv glucose, Parenteral glucagon
  7. Lipohypertrophy at injection site
  8. Allergic
  9. Hypo K - K shifts in to cells with insulin = hypo in blood
  10. DVD - Hypogly or hypergly (glucocorticoid)
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37
Q

Oral Anti-Diabetic drugs

A

Mostly for Type 2 Either lowers liver prod of glucose or promotes release of insulin

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38
Q

Metformin

A
  1. Type: Biguanides - Anti-diabetic Drug
  2. Dose: ORAL
  3. Moa: Reduce liver production of glucose AND promote release of insulin
  4. Use: Type 2 Diabetes DRUG OF CHOICE
  5. Side Fx:
    1. GI,
    2. Lactic acidosis (rare),
    3. Prevent type 2,
    4. Gestational diabetes
    5. OK IN PREG,
    6. PCOS
  6. DVD: NO IMPAIRED RENAL FUNCTION
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39
Q

Glyburide

A
  1. Type: Sulfonylureas *(first type)(2nd gen)
  2. ORAL Diabetic drug
  3. MOA: Promote insulin release
  4. USE: Type 2 only
  5. Side Fx:
    1. Hypoglycemia,
    2. weight gain
    3. prolonged QT interval (CardioTOXIC)
  6. DVD: Hypo/hyper watch out
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40
Q

Rosiglitazone

A
  1. Type: Thiazolidinediones (GLITAZONES) ORAL Diabetic drug
  2. MOA: reduce glucose levels by decreasing insulin resistance (RECEPTORS)
  3. Use: Add on in TYPE 2 (with Metformin)
  4. RESTRICTED USE
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41
Q

Pioglitazone

A
  1. Type: Thiazolidinediones (GLITAZONES) ORAL Diabetic drug
  2. MOA: reduce glucose levels by decreasing insulin resistance (RECEPTORS)
  3. Use: Add on in TYPE 2 (with Metformin)
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42
Q

Repaglinide

A
  1. Type: Meglitinides (Glinides) ORAL Diabetic drug
  2. MOA: Increase insulin secretion
  3. Adverse: WELL TOLERATED, hypoglycemia
  4. DVD - do not use with GEMFIBROZOLE - impacts break down of Rep and decreases efficacy
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43
Q

Nateglinide

A
  1. Type: Meglitinides (Glinides) ORAL Diabetic drug
  2. MOA: Increase insulin secretion
  3. Adverse: WELL TOLERATED, hypoglycemia
  4. DVD - do not use with GEMFIBROZOLE - impacts break down of Rep and decreases efficacy
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44
Q

Acarbose

A
  1. Type: Alpha-glucosidase inhibitor ORAL Diabetic drug
  2. MOA: Delays absorption of carbs in SI
  3. Use: Type 2
  4. Side FX:
    1. Flautlence,
    2. cramps,
    3. GI pain and distention,
    4. borborygmus,
    5. D,
    6. LIVER DYSFUNCTION
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45
Q

Miglitol

A
  1. Type: Alpha-glucosidase inhibitor ORAL Diabetic drug
  2. MOA: slow carb digestion
  3. Use: Latino and African American populations
  4. Side Fx: Flatulence, GI pain, other GI effects NO LIVER DYSFUNCTION
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46
Q

PUD

A
  1. Peptic Ulcer Disease GI disorders (lower esophagus, stomach, duodenum) Erosion of gut wall = can lead to hemorrhage and perforation
  2. Cause: imbalance between mucosal and aggressive factors
  3. EXAMPLE: over prod of stomach acid, chronic inflammatory damage, poor protective mucous production
47
Q

Defensive factors of PUD

A
    • Mucus - barrier between pepsin/acid and cells of GI lining
  2. -Bicarbonate - secreted by cells in stomach and duod., Trapped between mucus layer to neutralize hydrogen ions that might penetrate
    • Blood flow - poor BF = ischemia, cell injury and vulerability to attack -
  4. Prostaglandins - secretion of mucus and bicarb
48
Q

Aggressive Factors of PUD

A
    • H. Pylori - gram. Neg bacillus, many have - most with PUD have, lives between cells and mucus, may promote gastric cancer -
  2. NSAIDS - inhibit prostoglandins, reduce BF, mucus and Bicarb -
  3. gastric acid - injures cells of the mucosa - direct, activates pepsin - indirect, Zollinger-Ellison syndrome -
  4. Pepsin - proteolytic enzyme in GI juice -
  5. Smoking - delays healing and ups chance for reoccurence
49
Q

Tx for PUD

A

Goals: - Alleviate Sx - Promote healing - Prevent Compx - Prevent recurrence NOT ABLE TO ALTER DISEASE PROCESS

50
Q

Clarithromycin

A
  1. Type: Antibiotic for PUD
  2. MOA: inhibits protein synthesis - highly effective
  3. Resistance is rising - troublesome (upwards of 20% in some areas)
  4. Side Fx: N/D/distortion of taste
51
Q

Amoxicillin

A
  1. Type: Antibiotic for PUD
  2. MOA: H. Pylori is highly sensitive to amoxicillin - disrupts cell wall Resistance low = 3%
  3. Note: neutral pH is best - give with reduction of gastric acidity EX omeprazole Side
  4. Fx: D!
52
Q

Bismuth compond

A
  1. Type: LIKE antibiotic
  2. MOA: disrupt cell wall = lysis and death, may prevent h pylori from adhering to gastric surface
  3. Side FX: HARMLESS black coloration to tongue and stool - TEACH
  4. DO NOT USE LONG TERM = neurologic injury
53
Q

Metronidazole

A
  1. Type: Antibiotic for PUD
  2. MOA: very effective but 40% of strains are now resistant
  3. Side Fx:
    1. N/Headache
    2. AVOID ALCOHOL - Disulfiram rxn can occur??
      1. Flushing, fast heartbeats, nausea, thirst, chest pain, vertigo, and low blood pressure
    3. AVOID IN PREGNANCY!
54
Q

Tetracycline

A
  1. Type: Antibiotic for PUD
  2. MOA: inhibitor of bacterial protein synthesis - highly active against H pylori - resistance is low (1%)
  3. DO NOT USE WITH PREGNANT and YOUNG CHILDREN (TEETH)
55
Q

Drug Selection for PUD

A
    • Antibiotics - with PUD and documented H. Pylori, addition of antisecretory agents -
  2. NSAID induced - Risk - over 60 years, history of ulcers, high-dose NSAID -
    1. PPI are preferred,
    2. Misoprostol effective but D!
    3. Histamine blockers can work
    4. DO NOT USE Antacids, sucralfate, and histamine 2 receptor blockers
56
Q

Antibiotic regimen

A

Use at least 2 Add PPI or Histamine2RA (antisecretory) 10 day good, 14 day BETTER

57
Q

Cimetidine

A
  1. Type: Histamine2-Receptor Antagonists 1ST CHOICE FOR GASTRIC AND DUODENAL
  2. MOA: suppress secretion of gastric acid
  3. Dose: slow absorption with meals
  4. Use:
    1. GERD,
    2. Zollinger-Ellison,
    3. Aspiration pneumonitis,
    4. heartburn,
    5. acid indigestion,
    6. sour stomach
    7. Very difficult cross BBB
  5. No serious side Fx - some CNS effects (Antiandrogenic fx), CNS effects, Pneumonia, IV bolus - hypotension and dysrhythmia
  6. DVD: Warfarin, Phenytoin, theophylline, lidocaine, Antacidsd can reduce absorption (admin 1 hour apart)
58
Q

Ranitidine

A
  1. Type: Histamine2-Receptor Antagonists Similar to Cimetidine MORE POTENT FEWER DVD
  2. USE: short term treatment of gastric/duodenal, prophylaxis of duodenal ulcers, Zollinger-Ellison, Gerd Adverse
  3. fx: uncommon, does not bind to androgen receptors, elevation of gastric pH may increase risk of pneumonia
59
Q

Famotidine

A
  1. Type: Histamine2-Receptor Antagonists Similar to ranitidine
  2. USE: short - gastric/duod, Prophylaxis of RECURRENT duod, ZE syndrome, GERD, OTC - heart burn, acid stomach, sour stomach
  3. ADVERSE: NO antiadrogenic effects, possible pneumonia caused by elevated pH
60
Q

Nizatidine

A
  1. Type: Histamine2-Receptor Antagonists See ranitidine and famotidine
  2. USE: duodenal/gastric ulcers, GERD, heartburn, acid indigestion, sour stomach
61
Q

Omeprazole

A
  1. Type: PPI most effective acid suppressor
  2. MOA: inhibits gastric secretion, short half life
  3. USE: short term therapy - Gastric/duodenal ulcers and GERD, prophylaxis - only for pts in intensive care units (additional risk factors - multiple trauma, spinal cord injury and prolonged mechanical ventilation)
  4. Side Fx: headache, GI, pneumonia, fractures, hypomagnesemia, rebound acid hypersecretion, C Diff, Gastric cancer
62
Q

Esomeprazole

A

See Omeprazole Use: EROSIVE esophagitis, GERD, duodenal ulcers (H Pylori), prophylaxis of NSAID induced ulcers Adverse: H/D/N/flatulence, abdominal pain, dry mouth, pneumonia, hypomagnesemia, osteoporosis, fractures

63
Q

Lansoprazole

A

See omeprazole Adverse: D/GI pain/N, pneumonia, hypomagnesemia, osteoporosis, fracture

64
Q

Dexlansoprazole

A

MOA: Reduces gastric acidity by inhibiting gastric H+, K+, ATPase Use: Tx of erosive esophagitis, Tx of symptomatic GERD Adverse: D/GI pain/N/V/flatulence, URI, hypomag, osteoporosis, fractures

65
Q

Rabeprazole

A

See omeprazole and lansoprazole Use: H Pylori eradication, duodenal ulcers, GERD, hypersecretory states MOA: reduces gastric acidity by H+, K+, ATPase

66
Q

Pantoprazole

A

See Omeprazole and PPI USE: Gerd and hypersecretory Adverse: ORAL - D/H/Dizzy IV: D/H/N, dypepsia, inj site issues, Long term: hypomagnesemia, osteoperosis, fractures

67
Q

Sucralfate

A

Type: Mucosal Protectant MOA: barrier in gut for up to 6 hours USE: Acute ulcers and maintenance therapy Adverse Fx; Constipation (2%) DVD: Antacids may interfere

68
Q

Misopristol

A

Type: Antisecretory AND defense booster USE: ONLY for NSAID ulcers Adverse: Dose related diarrhea and GI pain Contraindicated during pregnancy - category X

69
Q

Mag Hydroxide (Milk of Mag, MAALOX)

A

Type: Antacid OF CHOICE MOA: Rapid acting, high ANC, long lasting, rxn with acid = neutral or low acid salts, also enhance mucosal protection by stimulating PROSTOGLANDINS Does not alter systemic ph CAUTION IN RENAL IMPAIRMENT (Mg difficult to regulate) AND UNDIAGNOSED ABDO PAIN Adverse: DIARRHEA, sodium loading DVD: Cimetidine, Ranitidine, Sucralfate??? Take with Al Hydrox = neutral diarr/constipation

70
Q

Al Hydroxide

A

Type: Antacid MOA: low ANC, slow, long duration, not used alone, rxn with acid = neutral or low acid salts, also enhance mucosal protection by stimulating PROSTOGLANDINS Does not alter systemic ph CAUTION IN RENAL IMPAIRMENT Adverse: CONSTIPATION, HIGH SODIUM DVD: Tetracycline, warfarin, digoxin

71
Q

Calcium Carbonate

A

Type: Antacid MOA: rapid acting, high ANC, long duration Adverse: Constipation, eructation (belching) and flatulence, low palatability

72
Q

Cholinergic Drugs

A

Muscarinic Agonist Muscarinic ANTAG Cholinesterase inhibitor Nicotinic Drugs

73
Q

Adrenergic Drugs

A

Adrenergic AGONIST Adrenergic ANTAGONIST Indirect Anti-adrenergic Agent

74
Q

Cholinergic (ADH) Receptors

A

N1 - Skeletal Muscle N2 - Autonomic Ganglionic (Symp/Parasymp - ignore) M1 - CNS M2 - Heart, smooth muscle M3 - Glands, smooth muscle

75
Q

ACH effects by system

A

Cardio: Vasodilation, Decreased HR, Decreased contractile force Resp: Bronchoconstriction, Up airway secretions Urinary: Bladder contraction = PEE GI tract: up motility and secretion = POOP Other: General increase in secretions, Miosis - pupillary constriction

76
Q

Muscarinic Agonist Overdose

A

Source: Mushrooms, od on muscarinic agonist, ACHesterase inhibitor S/Sx: Salivation, tearing, visual disturbances, bronchospasm, diarrhea, bradycardia, hypotension Tx: ATROPINE

77
Q

Bethanechol

A

Type: Muscarinic AGONIST (Parasympathomimetic) MOA: Selective blockade of muscarinic receptors Effects: Heart - Bradycardia, Lung - constriction, GI - Increased tone and motility, Bladder - Contraction of detrusor and relax of trigone and sphincter, Exocrine - sweat, salivate, bronchial secretions and secrete gastric acid USE: URINARY RETENTION and id gi issues Adverse: Hypotension, Asthma exacerbation, dysrhythmia in hyperTHYROIDISM,

78
Q

Pilocarpine

A

Type: Muscarinic Agonist Use: Xerostomia (dry mouth) from head/neck radation, Sjogren’s syndrome, DROPS for glaucoma and as miotic agent (PUPIL shrink)

79
Q

Atropine

A

Type: Muscarinic ANTAG (Anticholinergic) *Best known (found in nature cows eating clover, suicide attempt) MOA: Muscarinic receptor blockade Effects on systems: HR UP, Secretions DOWN, Lungs OPEN, Bladder HOLDS, GI HOLDS, Eyes - Mydriasis (dialated pupils) and cycloplegia (paralyzed muscle for focusing), CNS - hallucinations/delirium USE: preanesthetic, disorders of the eye, bradycardia, GI hyper, muscarinic agonist poisoning, PUD, Asthma, Biliary colic Adverse: Xerostomia, Blurred vision, Photophobia, UP IOP, urinary retention, constipation, Anhidrosis (inability to sweat), tachycardia, asthma DVD: NO other muscarinic blockades Dose: Systemic therapy, Atropen for cholinesterase inhibitor poisoning, opthalmology (dilating)

80
Q

Oxybutynin

A

Type: Muscarinic ANTAG (Anticholinergic) Use: OVERACTIVE BLADDER (1/3 USA, Behavioral and drug) (Last resort - percutaneous tibial nerve stimulation) Dose: Syrup, extended release, transdermal patch/gel MOA: M3 receptors Fx: Anticholinergic side fx common

81
Q

Scopolamine

A

Type: Muscarinic ANTAG (Anticholinergic) Like Atropine Effects: SEDATION Use: Anti-emetic and Motion Sickness, cycloplegia and mydriasis for opthamology, preanesthetic sedation

82
Q

Ipratropium Bromide

A

Type: Muscarinic ANTAG (Anticholinergic) USE: Asthma, COPD, rhinitis Dose: Inhalation - not associated with antiACH side effects (ex dry mouth, blurred vision, urinary hesitancy and C)

83
Q

Antimuscarinic OD

A

S/Sx: Dry mouth, blurred vision, photophobia, hypertermia, CNS effects, Hot/dry/flushed Tx: PHYSOSTIGMINE (ACHesterase inhibitor) DIFF B/T poison and PSYCHOTIC EPI

84
Q

ACHesterase Inhibitors

A

ACHesterase - breaks down ACH Inhibitor - no break down = more ACH in system = more rest and digest USE: myasthenia gravis - receptor

85
Q

Neostigmine

A

Type: ACHesterase inhib - PROTOTYPIC Moderate duration, Reversible MOA: Effects Muscarinic receptors and NMJ (not ganglionic or CNS) OD: suppress CNS (respiration) Dose: ORAL or IM - poor oral absorbtion (post charge) Contraindicated in patients on NMJ blockers (succinylcholine) - intensify

86
Q

Physostigmine

A

Type: ACHesterase inhib DRUG OF CHOICE FOR ATROPINE POISONING and other muscarinic blockers Uncharged - cross BBB DVD: Alzheimer’s disease drugs

87
Q

Edrophonium

A

Type: Fast acting ACHesterase inhibitor Test during crisis DOSE - better = Myasthenic DOSE - worse = cholinergic

88
Q

Myasthenia Gravis

A

Process: Autoimmune - antibodies attack N1 receptors on skeletal muscle = great weakness S/Sx: Ptosis (drooping eyelids), dysphagia, weakness of skeletal muscle Tx: symptom treatment with ACHesterase inhibitors = more ACH to the nicotinic receptor = more ennervation of skeletal muscles Side Fx: Too much, Atropine to reverse Dose: start small, keep track of time, strength, time to fatigue, signs of over dose - learn to dose in anticipation of exercise etc

89
Q

Cholinergic Crisis

A

TOO MUCH DRUG -weakness, paralysis Tx - respiratory support and atropine

90
Q

Myasthenic crisis

A

NOT ENOUGH DRUG - weakness Tx - more drug

91
Q

Dopamine

A

Type: Adrenergic AGONIST MOA: Direct binding to Adrenergic receptor SPECIFICITY: A1, B1, B2, Dopaminergic USE: SHOCK (Dilation of the renal bv reduces risk of renal failure), enhances cardiac performance Dose: Low - Dopamine, Moderate - Dopa and B1, High - Dop, A1, B1 Use: Shock - increase cardiac output, increase renal perfusion, Heart failure - increase myocardial contractility

92
Q

Epinephrine

A

Type: Adrenergic AGONIST (Catecholamine) MOA: direct binding SPECIFICITY: A1, A2, B1, B2 USE: Anaphylaxis!, delays absorption of local anesthetic, controls bleeding, Up BP, Overcome AV block, restores cardiac funcx, Bronchial dilation, DOSE: IM, SQ, IV, short half life ADVERSE: hypertensive crisis - cerebral hemorrhage, dysrhythmias - CAUTION in HYPERTHYROIDISM - sensitive = high risk DVD: MAO inhib - MAO inactivate epi and cate., MAO inhib - intensifies, TCA - block uptake = prolongs/intensifies effect Dose; Pen, IV (clos monitor), IM, SQ, Intracardiac, Intraspinal, Inhalation, Topical

93
Q

Isoproterenol

A

Type: Adrenergic AGONIST *Catecholamine MOA: Direct binding SPECIFICITY: B1, B2 Use: AV heart block, Cardiac arrest, Increase cardiac output in shock ADVERSE: fewer than epi (no alph-adrenergic receptors) Dose: IV, IM, Intracardiac

94
Q

Dobutamine

A

Type: Adrenergic AGONIST *Catecholamine SPECIFICITY: B1 Use: CHF DOSE: Continuous IV

95
Q

Ephedrine

A

Type: Adrenergic AGONIST MOA: direct bind AND promotion of NE release SPECIFICITY: A1, A2, B1, B2 MIXED ACTING USE: Asthma, Shock, Anesthesia induced hypotension Contraindicated: BREAST FEED Side Fx: loss of app, (short term weightloss)

96
Q

Phenylephrine

A

Type: Adrenergic AGONIST SPECIFICITY: A1 Use: Reduce nasal cong (locally), Up BP (parenteral), dilates pupils (eye), Local anesthetic (delays absorption)

97
Q

Terbutaline

A

Type: Adrenergic AGONIST SPECIFICITY: B2

98
Q

Prazosin

A

Type: Alpha Adrenergic ANTAG SPECIFICITY: A1 MOA: Comp. Antag Effect: Dilation of arterioles and viens, relax smooth muscle in bladder and prostate, USE: HTN only Dose: Oral - 1-3 hours post dose peak, last for 10 Caution; Metabolized in liver

99
Q

Tamulosin

A

Type: Alpha Adrenergic ANTAG SPECIFICITY: A1 Action: selective blockade - bladder neck, prostatic cap, urethra, USE: BPH Adverse: HEadache, dizzy, rhinitis, abnormal ejaculation

100
Q

Phentolamine

A

Type: Alpha Adrenergic ANTAG SPECIFICITY: NON-selective A1, A2 MOA: Comp antag. USE: Dx and tx of pheochromocytoma (CATECHOLAMINE SECRETING TUMOR), treat extravasation of alpha1 vasoconstriction, reversal of soft tissue anethesia Adverse: Orthostatic hypotension, reflex tachy

101
Q

Propranolol

A

Type: BETA Adrenergic ANTAG SPECIFICITY: NON selective - B1, B2 Effects - reduced CO, block renin, bronchoconstriction, vasoconstriction, down glycogenolysis Metab: widely distributed USE: HTN, Angina, MI Adverse: Bradycardia, AV heart block, Heart failure, Reboud tachy DVD: CA blockers, Insulin Dose: difficult, Oral IV ALLERGY, NOT WITH DIABETES, NOT WITH CARDIAC, RESPIRATORY or PSYCH DISORDERS

102
Q

Metropolol

A

Type: BETA Adrenergic Antag SPECIFICITY: B1 2nd gen Better for PTs with diabetes or Asthma USE: HTN, Angina Adverse - same but less bronchoconstriction NOT IN AV BLOCK 2,3, NOT IN Sinus Brady, Safer for asthma, safer in diabetes

103
Q

Labetalol

A

Type: BETA Adrenergic ANTAG SPECIFICITY: NON selective - B1 B2 AND alpha Adverse: Orthostatic hypo, Insomnia, depression, dilate BV

104
Q

Carvedilol

A

Type: BETA Adrenergic ANTAG SPECIFICITY: NON selective - B1 B2 AND alpha Adverse: Orthostatic hypo, Insomnia, depression, dilate BV

105
Q

Adrenergic Receptors

A

A1 - Constriction of BV, Contraction of smooth muscles, Increased Glucose Metabolism A2 - regulates amount reaching A1 B1 - Heart, Up Renin release from juxtaglomerular cells, Up hunger B2 - smooth muscle relaxation, contract urethral sphyncter, Up renin, Up glucose metabolism, Lipolysis, Thick saliva

106
Q

Alpha 1 Activation

A

Hemostasis, Nasal decongestant, Delays absorption of local anesthetic, Elevate blood pressure, Mydriasis DRUGS: Epi, Norepi, Phenylephrine, Dopamine

107
Q

Alpha 2 activation

A

Reduce sympathetic outflow to heart - ANTI-HTN, Relief of severe pain EX Clonidine

108
Q

Beta 1 activation

A

On heart Drugs: Epi, NE, Isoproterenol, dopamine, dobutamine, ephedrine Use: Shock, hyptension/reduced perfusion, Maintain BF, Heart failure, Heart block (temporary), acute resuscitation from MI (EPINEPHRINE) ADVERSE: Dysrhythmia, Angina Pectoris (esp with coronary circ issues)

109
Q

Beta 2 Activation

A

Lungs and Uterus DRUGS: Ephinephrine, Isoproterenol, Albuterol USE: Asthma, delay preterm labor, hyperglycemia (liver) Adverse: Tremor (initiate at low doses to prevent)

110
Q

Albuterol

A

Adrenergic AGONIST *NONcatecholamine Specificity: B2 USE: Asthma Adverse: not much, high dose - b1 receptor, tremor, tachycardia

111
Q

Alpha BLOCKADE Benefits

A
  • Essential HTN (A1), OD - Phentolamine for Extravasated necrosis - BPH - reduce contraction of smooth muschle in prostatic capsule and bladder - Pheochromocytoma - Catecholamine secreting tumor in adrenal medula - Raynaud’s disease - keep vessels open
112
Q

Alpha BLOCKADE Cons

A
  • A2 effects are low - Orthostatic Hypotension -Reflex Tachy - Nasal congestion - A2 (reflex tachy, baroreceptor reflex)
113
Q

Beta BLOCKADE Benefits

A

-Angina pectoris - HTN - dysrhythmias -MI - HYPERthyroid - Migrane - reduce frequency and intensity - Pheochromocytom - Glaucoma

114
Q

Beta BLOCKADE adverse

A
  • non selective - broad neg effects - Bradycardia - Down CO - Heart Failure - Rebound cardiac excitation - Bronchoconstriction - Hypoglycemia (inhibit glycogenolysis) - Adverse in neonates

PhArmacology 101 (4 decks)

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