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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
Pre diabetes
impaired fasting glucose - 100-125 many people never develop
26
Tx DM
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
27
Glucose target
1. Pre meal: 70-130 2. Post meal: 100-140 3. A1C test: usual human = 7% but DM human = 8% to avoid hypoglycemic attack
28
Insulin
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
29
Insulin ASPART
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
30
Insulin LISPRO
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
31
Insulin GLULISINE
1. Rapid onset (10-15mins) 2. Short duration (3-5hours) 3. Synthetic analog of human 4. Dose: near time of eating
32
Regular insulin
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
33
NPH insulin
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
34
Insulin GLARGINE
Duration: 24 hours Dose: 1x daily T1 (kids and adult) T2 (adult) SubQ
35
Dosing schedule of Insulin
1. - Twice daily premixed 2. - Intensive basal/bolus strategy 3. - continous subcutaneous insulin
36
Complications of Insulin
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)
37
Oral Anti-Diabetic drugs
Mostly for Type 2 Either lowers liver prod of glucose or promotes release of insulin
38
Metformin
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
39
Glyburide
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
40
Rosiglitazone
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
41
Pioglitazone
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)
42
Repaglinide
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
43
Nateglinide
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
44
Acarbose
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
45
Miglitol
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
46
PUD
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
Defensive factors of PUD
1. - 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 3. - Blood flow - poor BF = ischemia, cell injury and vulerability to attack - 4. Prostaglandins - secretion of mucus and bicarb
48
Aggressive Factors of PUD
1. - 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
Tx for PUD
Goals: - Alleviate Sx - Promote healing - Prevent Compx - Prevent recurrence NOT ABLE TO ALTER DISEASE PROCESS
50
Clarithromycin
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
Amoxicillin
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
Bismuth compond
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
Metronidazole
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
Tetracycline
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
Drug Selection for PUD
1. - 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
Antibiotic regimen
Use at least 2 Add PPI or Histamine2RA (antisecretory) 10 day good, 14 day BETTER
57
Cimetidine
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
Ranitidine
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
Famotidine
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
Nizatidine
1. Type: Histamine2-Receptor Antagonists See ranitidine and famotidine 2. USE: duodenal/gastric ulcers, GERD, heartburn, acid indigestion, sour stomach
61
Omeprazole
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
Esomeprazole
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
Lansoprazole
See omeprazole Adverse: D/GI pain/N, pneumonia, hypomagnesemia, osteoporosis, fracture
64
Dexlansoprazole
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
Rabeprazole
See omeprazole and lansoprazole Use: H Pylori eradication, duodenal ulcers, GERD, hypersecretory states MOA: reduces gastric acidity by H+, K+, ATPase
66
Pantoprazole
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
Sucralfate
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
Misopristol
Type: Antisecretory AND defense booster USE: ONLY for NSAID ulcers Adverse: Dose related diarrhea and GI pain Contraindicated during pregnancy - category X
69
Mag Hydroxide (Milk of Mag, MAALOX)
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
Al Hydroxide
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
Calcium Carbonate
Type: Antacid MOA: rapid acting, high ANC, long duration Adverse: Constipation, eructation (belching) and flatulence, low palatability
72
Cholinergic Drugs
Muscarinic Agonist Muscarinic ANTAG Cholinesterase inhibitor Nicotinic Drugs
73
Adrenergic Drugs
Adrenergic AGONIST Adrenergic ANTAGONIST Indirect Anti-adrenergic Agent
74
Cholinergic (ADH) Receptors
N1 - Skeletal Muscle N2 - Autonomic Ganglionic (Symp/Parasymp - ignore) M1 - CNS M2 - Heart, smooth muscle M3 - Glands, smooth muscle
75
ACH effects by system
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
Muscarinic Agonist Overdose
Source: Mushrooms, od on muscarinic agonist, ACHesterase inhibitor S/Sx: Salivation, tearing, visual disturbances, bronchospasm, diarrhea, bradycardia, hypotension Tx: ATROPINE
77
Bethanechol
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
Pilocarpine
Type: Muscarinic Agonist Use: Xerostomia (dry mouth) from head/neck radation, Sjogren’s syndrome, DROPS for glaucoma and as miotic agent (PUPIL shrink)
79
Atropine
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
Oxybutynin
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
Scopolamine
Type: Muscarinic ANTAG (Anticholinergic) Like Atropine Effects: SEDATION Use: Anti-emetic and Motion Sickness, cycloplegia and mydriasis for opthamology, preanesthetic sedation
82
Ipratropium Bromide
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
Antimuscarinic OD
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
ACHesterase Inhibitors
ACHesterase - breaks down ACH Inhibitor - no break down = more ACH in system = more rest and digest USE: myasthenia gravis - receptor
85
Neostigmine
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
Physostigmine
Type: ACHesterase inhib DRUG OF CHOICE FOR ATROPINE POISONING and other muscarinic blockers Uncharged - cross BBB DVD: Alzheimer’s disease drugs
87
Edrophonium
Type: Fast acting ACHesterase inhibitor Test during crisis DOSE - better = Myasthenic DOSE - worse = cholinergic
88
Myasthenia Gravis
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
Cholinergic Crisis
TOO MUCH DRUG -weakness, paralysis Tx - respiratory support and atropine
90
Myasthenic crisis
NOT ENOUGH DRUG - weakness Tx - more drug
91
Dopamine
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
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Epinephrine
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
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Isoproterenol
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
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Dobutamine
Type: Adrenergic AGONIST \*Catecholamine SPECIFICITY: B1 Use: CHF DOSE: Continuous IV
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Ephedrine
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)
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Phenylephrine
Type: Adrenergic AGONIST SPECIFICITY: A1 Use: Reduce nasal cong (locally), Up BP (parenteral), dilates pupils (eye), Local anesthetic (delays absorption)
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Terbutaline
Type: Adrenergic AGONIST SPECIFICITY: B2
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Prazosin
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
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Tamulosin
Type: Alpha Adrenergic ANTAG SPECIFICITY: A1 Action: selective blockade - bladder neck, prostatic cap, urethra, USE: BPH Adverse: HEadache, dizzy, rhinitis, abnormal ejaculation
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Phentolamine
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
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Propranolol
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
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Metropolol
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
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Labetalol
Type: BETA Adrenergic ANTAG SPECIFICITY: NON selective - B1 B2 AND alpha Adverse: Orthostatic hypo, Insomnia, depression, dilate BV
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Carvedilol
Type: BETA Adrenergic ANTAG SPECIFICITY: NON selective - B1 B2 AND alpha Adverse: Orthostatic hypo, Insomnia, depression, dilate BV
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Adrenergic Receptors
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
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Alpha 1 Activation
Hemostasis, Nasal decongestant, Delays absorption of local anesthetic, Elevate blood pressure, Mydriasis DRUGS: Epi, Norepi, Phenylephrine, Dopamine
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Alpha 2 activation
Reduce sympathetic outflow to heart - ANTI-HTN, Relief of severe pain EX Clonidine
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Beta 1 activation
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)
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Beta 2 Activation
Lungs and Uterus DRUGS: Ephinephrine, Isoproterenol, Albuterol USE: Asthma, delay preterm labor, hyperglycemia (liver) Adverse: Tremor (initiate at low doses to prevent)
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Albuterol
Adrenergic AGONIST \*NONcatecholamine Specificity: B2 USE: Asthma Adverse: not much, high dose - b1 receptor, tremor, tachycardia
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Alpha BLOCKADE Benefits
- 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
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Alpha BLOCKADE Cons
- A2 effects are low - Orthostatic Hypotension -Reflex Tachy - Nasal congestion - A2 (reflex tachy, baroreceptor reflex)
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Beta BLOCKADE Benefits
-Angina pectoris - HTN - dysrhythmias -MI - HYPERthyroid - Migrane - reduce frequency and intensity - Pheochromocytom - Glaucoma
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Beta BLOCKADE adverse
- 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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