IV - DRUGS FOR SMOOTH MUSCLE

Question 1

more likely to block autonomic receptors, also has alpha1 blocking and local anesthetic effect

Answer 1

1st Generation antihistamines DIPHENHYDRAMINE [B], BROMPHENIRAMINE [C], CHLORPHENIRAMINE [B], CYCLIZINE [B], MECLIZINE [B], BUCLIZINE [C], CARBINOXAMINE [C], DIMEHYDRINATE [B], HYDROXYZINE [C], PROMETHAZINE [C], CYPROHEPTADINE [B], CLEMASTINE [B], TRIPELENNAMINE [B]

Question 2

Reversible blockade of histamine H1-receptor sites on tissues, No sedation and antimuscarinic effects

Answer 2

2nd Generation antihistamines CETIRIZINE, LORATADINE [B], FEXOFENADINE [C], DESLORATADINE [C], LEVOCETIRIZINE [B], TERFENADINE [C], ASTEMIZOLE [C], EBASTINE, AZELASTINE [C], BILASTINE, RUPATADINE [B]

Question 3

No sedation and antimuscarinic effects.
No autonomic or anti-motion sickness effects.
Can cause fatal arrythmias from interaction between azoles/erythromycin and Terfenadine/ Astemizole.

Answer 3

2nd Generation H1 receptor blockers

Question 4

reduction of nocturnal acid secretion in gastirc and duodenal ulcer

Answer 4

H2 antagonists
CIMETIDINE, RANITIDINE, FAMOTIDINE, NIZATIDINE

(TOPNOTCH)

Question 5

True or False: H2 antagonists have H1-blocking effect

Answer 5

FALSE (TOPNOTCH)

Question 6

True or False: Ranitidine is a CYP450 inhibitor

Answer 6

TRUE, but weak inhibitor only (TOPNOTCH)

Question 7

Agonist at the 5HT1D receptor in the blood vessels causing vasocontriction ; 1st line treatment for Acute migraine and cluster headache attacks

Answer 7

5HT1D receptor agonist: Sumatriptan, Naratriptan, Almotriptan, Eletriptan, Frovatriptan, Rizatriptan, Zolmitriptan (TOPNOTCH)

Question 8

Selectively block 5HT3 receptors ; For antiemesis in patients post-chemotherapy or post-operation

Answer 8

5HT3 receptor antagonist: Ondansetron, Granisetron, Dolasetron, Alosetron (TOPNOTCH)

Question 9

can inc QRS and QT (proarrhythmic effect) duration so never use in patients with heart disease

Answer 9

Dolasetron (TOPNOTCH)

Question 10

• Partial agonist at a and 5-HT 2 receptors, some have potent agonist effect at Dopamine receptors
• Gastrointestinal upset, Vasospasm, Gangrene, Uterine spasm, Retroperitoneal fibrosis (methysergide only)

Answer 10

Ergotamine, DIHYDROERGOTAMINE [X], METHYSERGIDE [X]

5-HT2 -receptor antagonist (vasoselective)

Antidote is Nitroprusside

Question 11

uterus becomes more sensitive to ergots during pregnancy, produce very powerful and long-lasting contraction leading to decreased bleeding, Never give before delivery of placenta

Answer 11

Ergonovine - 5-HT2 -receptor antagonist (uteroselective)

Question 12

PGE1 analogue, causes increased HCO3 and mucus secretion in stomach and uterine contraction

Answer 12

Misoprostol, Gemeprost (TOPNOTCH)

Question 13

may also be used together with Mifepristone or Methotrexate as safe abortifacient

Answer 13

Misoprostol (TOPNOTCH)

Question 14

Low concentrations contract, higher concentrations relax uterine and cervical smooth muscle, soften cervix at term before induction with oxytocin

Answer 14

PGE2analogDinoprostone, Sulprostone (TOPNOTCH)

Question 15

PGF2a analogue, increases outflow of aqueous humor thus reduces intraocular pressure; For glaucoma

Answer 15

Prostaglandin F2a analog: Latanoprost, Arboprost, Bimatoprost, Travoprost, Unoprostone (TOPNOTCH)

Question 16

used primarily for pulmonary hypertension

Answer 16

Prostaglandin I2 analog
“BITE”

Beraprost, Iloprost, Treprostinil, Epoprostenol

Question 17

SE: Tachycadia, Nervousness, tremors, restlessness, arrythmias when used excessively, loss of responsiveness (tolerance, tachyphylaxis)

Answer 17

Beta2-selective agonist (short-acting): Albuterol/Salbutamol, Levalbuterol, Terbutaline, Metaproterenol, Pirbuterol, Procaterol, Fenoterol (TOPNOTCH)

Question 18

Increase asthma mortality when used alone; May precipitate arrhytmias; usual DOA: 12hrs

Answer 18

Beta2-selective agonist (long acting): Salmeterol, Formoterol, Cleneterol, Bambuterol (TOPNOTCH)

Question 19

More effective and less toxic than beta agonists ith COPD

Answer 19

Muscarinic receptor antagonist: Ipratropium, Tiotropium (TOPNOTCH)

Question 20

Phosphodiesterase inhibitor, Adenosine receptor antagonist, causes bronchodilation and inc. strength of contraction of diaphragm; For asthma esp in nocturnal attacks

Answer 20

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

Question 21

Antidote in overdosage is BB. Higher clearance in adolescents and smokers. Narrow therapeutic window

Answer 21

Methylxanthines: Theophylline, Aminophylline, Pentoxifylline (TOPNOTCH)

Question 22

Prevents calcium influx and stabilizes mast cells, preventing degranulation and release of histamine, leukotrienes and mediators; for Asthma prophylaxis and allergies

Answer 22

Mast cell Stabilizer: Cromolyn, Nedocromil, Lodoxamide (TOPNOTCH)

Question 23

DOC for Asthma prophylaxis, First line treatment for moderate to severe BA, COPD

Answer 23

Corticosteroid: Fluticasone, Beclomethasone, Budesonide, Flunisolide, Mometasone, Triamcinolone, Ciclosenide (TOPNOTCH)

Question 24

For status asthmaticus

Answer 24

use IV prednisolone or hydrocortisone (TOPNOTCH)

Question 25

active metabolite of prednisone

Answer 25

prednisolone (TOPNOTCH)

Question 26

Inhibitor of 5-lipoxygenase. Reduces synthesis of leukotrienes. Prevents airway inflammation and bronchoconstriction; For asthma prophylaxis

Answer 26

Zileuton

• No bronchodilator actions. Not recommended for acute BA attack. The Lukasts gained more popularity because this group of LT inhibitors can cause transaminitis

Question 27

No bronchodilator action, not recommended for acute BA attack

Answer 27

Zileuton, Montelukast, Zafirlukast, Pranlukast (TOPNOTCH)

Question 28

Binds IgE antibodies on sensitized mast cells and prevents activation by BA triggers and subsequent release of inflammatory mediators; For prophylaxis of severe, refractory asthma not responsive to all other drugs

Answer 28

Anti-IgE antibody: Omalizumab (TOPNOTCH)