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immunopharmacology > Smooth muscle relaxants used for relief GI and UG spasms. Drugs influencing uterus functions. Antihistamines H1-blocker > Flashcards

Smooth muscle relaxants used for relief GI and UG spasms. Drugs influencing uterus functions. Antihistamines H1-blocker Flashcards

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1
Q

Agents used

A

papaverine.
drotaverine. butylscopolamine. misoprostol.
oxytocin.
ergotamine.
terbutaline.
atosiban.
Mg++.
ethanol .
solifenacin.
oxybutinine.
tamsulosin.

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2
Q

Histamine

A

Organic, nitrogen-containing compound; classified as amine autacoid (physiologically active metabolite, released by specific cells and tissues, having short-lasting and local effects)

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3
Q

▪ Cells with histamine synthesis and storage properties

A
  • CNS neurons (role in sleep-arousal regulation)
  • Enterochromaffin cells
  • Mast cells
  • Basophils, eosinophils
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4
Q

H1

A

H1

Smooth muscle
Endothelium
Brain

Gq

  • Capillary dilation (via NO) → BP ↓
  • Capillary permeability → tissue edema
  • Bronchiolar smooth muscle contraction
    (bronchoconstriction)
  • Activation of peripheral nociceptive
    receptors → pain and pruritus
  • Nasal and bronchial mucous secretion ↑
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5
Q

H2

A

H2

Gastric mucosa
Cardiac muscle
Mast cells
Brain

Gs

  • Gastric acid secretion ↑
  • Cardiac stimulant effect: SA nodal rate
    and automaticity ↑, positive inotropic
  • Negative feedback effect – reduce
    histamine release from mast cells
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6
Q

H3

A

H3

Presynaptic receptors in the CNS and periphery

Gi

  • Presynaptic modulation of histaminergic neurons in the CNS and the periphery
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7
Q

H4

A

H4

Eosinophils
Neutrophils
CD4+ T-cells

Gi

  • Chemotactic response in leukocyte (especially eosinophils) and mast cells
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8
Q

Antihistamines

A

H1 receptor antagonists – 1st gen’:
Diphenhydramine
Promethazine
Dimetindene

H1 receptor antagonists – 2nd gen’
Cetirizine
Loratadine
Fexofenadine

H2 receptor antagonists
Cimetidine
Ranitidine
Famotidine
Nizatidine
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9
Q

H1 receptor antagonists – 1st gen’

A
  • Competitive inhibitors of central and peripheral H1 receptors
  • α-adrenergic receptor inhibition properties
  • M-cholinergic receptor inhibition properties
  • Serotonin receptor inhibition properties (only a few agents)

Diphenhydramine
Promethazine
Dimetindene

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10
Q

Diphenhydramine

A

H1 receptor antagonists – 1st gen’

  • Competitive inhibitors of central and peripheral H1 receptors
  • α-adrenergic receptor inhibition properties
  • M-cholinergic receptor inhibition properties
  • Serotonin receptor inhibition properties (only a few agents)
  • Oral or parenteral
  • Duration of action 4-12 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Lipophilic (easily cross the blood-brain-barrier)
  • IgE-mediated allergies (ex. hay fever, urticaria)
  • Sedative (ex. preoperative sedation)
  • Antiemetic (ex. chemotherapy-induced vomiting)
  • Sleep-aid formulations (over the counter drug)
  • Anti-motion sickness
  • Control of nausea and vomiting of pregnancy
    (in combination with pyridoxine - B6 vitamin)
  • Management of acute extrapyramidal symptoms
    (ex. due to antipsychotics)
  • Side effects: sedation, antimuscarinic effects
    (dry mouth, blurred vision, glaucoma exacerbation), α-adrenoreceptor inhibitory effects (orthostatic hypotension)
  • Interactions: additive sedation with other sedatives (BZD, alcohol)
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11
Q

Promethazine

A

H1 receptor antagonists – 1st gen’

  • Competitive inhibitors of central and peripheral H1 receptors
  • α-adrenergic receptor inhibition properties
  • M-cholinergic receptor inhibition properties
  • Serotonin receptor inhibition properties (only a few agents)
  • Oral or parenteral
  • Duration of action 4-12 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Lipophilic (easily cross the blood-brain-barrier)
  • Less anti-motion sickness effect
  • More sedative and autonomic effects
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12
Q

Dimetindene

A

H1 receptor antagonists – 1st gen’

  • Competitive inhibitors of central and peripheral H1 receptors
  • α-adrenergic receptor inhibition properties
  • M-cholinergic receptor inhibition properties
  • Serotonin receptor inhibition properties (only a few agents)
  • Oral or parenteral
  • Duration of action 4-12 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Lipophilic (easily cross the blood-brain-barrier)
  • Symptomatic treatment of allergic reactions
  • Minimally crosses blood-brain-barrier → milder side
    effects with efficient control of allergies
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13
Q

H1 receptor antagonists – 2nd gen’

A
  • Competitive inhibitors of peripheral H1 receptors
  • No autonomic or anti-motion sickness effect

Cetirizine
Loratadine
Fexofenadine

  • IgE-mediated allergies (hay fever, urticaria, angioedema)
  • Side effects (generally milder compared to 1st gen’): sedation, arrhythmias in overdose
  • Interactions: additive sedation with other sedatives (BZD, alcohol)
  • Much less lipophilic (less likely to cross the blood-brain-barrier)
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14
Q

Cetirizine

A

H1 receptor antagonists – 2nd gen’

  • Competitive inhibitors of peripheral H1 receptors
  • No autonomic or anti-motion sickness effect
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Much less lipophilic (less likely to cross the blood-brain-barrier)
  • IgE-mediated allergies (hay fever, urticaria, angioedema)
  • Side effects (generally milder compared to 1st gen’): sedation, arrhythmias in overdose
  • Interactions: additive sedation with other sedatives (BZD, alcohol)
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15
Q

Loratadine

A

H1 receptor antagonists – 2nd gen’

  • Competitive inhibitors of peripheral H1 receptors
  • No autonomic or anti-motion sickness effect
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Much less lipophilic (less likely to cross the blood-brain-barrier)
  • IgE-mediated allergies (hay fever, urticaria, angioedema)
  • Side effects (generally milder compared to 1st gen’): sedation, arrhythmias in overdose
  • Interactions: additive sedation with other sedatives (BZD, alcohol)
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16
Q

Fexofenadine

A

H1 receptor antagonists – 2nd gen’

  • Competitive inhibitors of peripheral H1 receptors
  • No autonomic or anti-motion sickness effect
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Much less lipophilic (less likely to cross the blood-brain-barrier)
  • IgE-mediated allergies (hay fever, urticaria, angioedema)
  • Side effects (generally milder compared to 1st gen’): sedation, arrhythmias in overdose
  • Interactions: additive sedation with other sedatives (BZD, alcohol)
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17
Q

H2 receptor antagonists

A
  • Competitive inhibitors of peripheral H2 receptors
  • No H1, autonomic or anti-motion sickness effects

Cimetidine
Ranitidine
Famotidine
Nizatidine

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18
Q

Cimetidine

A

H2 receptor antagonists

  • Competitive inhibitors of peripheral H2 receptors
  • No H1, autonomic or anti-motion sickness effects
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Acid peptic disease (duodenal and gastric)
  • Control of Zollinger-Allison syndrome (gastrin-secreting
    neuroendocrine tumor)
  • Gastroesophageal reflux disease (GERD)
  • Stress ulcers, mucosal erosion, gastric hemorrhage in
    ICU patients (given IV)
  • Not 1st-line agent in the reduction of gastric acidity! (initial approach is based on treatment with PPI’s)
  • Side effects: cimetidine (but not other agents) is a weak antiandrogenic agent and a potent P450 enzyme inhibitor
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19
Q

Ranitidine

A

H2 receptor antagonists

  • Competitive inhibitors of peripheral H2 receptors
  • No H1, autonomic or anti-motion sickness effects
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Acid peptic disease (duodenal and gastric)
  • Control of Zollinger-Allison syndrome (gastrin-secreting
    neuroendocrine tumor)
  • Gastroesophageal reflux disease (GERD)
  • Stress ulcers, mucosal erosion, gastric hemorrhage in
    ICU patients (given IV)
  • Not 1st-line agent in the reduction of gastric acidity! (initial approach is based on treatment with PPI’s)
  • Side effects: cimetidine (but not other agents) is a weak antiandrogenic agent and a potent P450 enzyme inhibitor
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20
Q

Famotidine

A

H2 receptor antagonists

  • Competitive inhibitors of peripheral H2 receptors
  • No H1, autonomic or anti-motion sickness effects
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Acid peptic disease (duodenal and gastric)
  • Control of Zollinger-Allison syndrome (gastrin-secreting
    neuroendocrine tumor)
  • Gastroesophageal reflux disease (GERD)
  • Stress ulcers, mucosal erosion, gastric hemorrhage in
    ICU patients (given IV)
  • Not 1st-line agent in the reduction of gastric acidity! (initial approach is based on treatment with PPI’s)
  • Side effects: cimetidine (but not other agents) is a weak antiandrogenic agent and a potent P450 enzyme inhibitor
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21
Q

Nizatidine

A

H2 receptor antagonists

  • Competitive inhibitors of peripheral H2 receptors
  • No H1, autonomic or anti-motion sickness effects
  • Oral or parenteral
  • Duration of action 12-24 h’
  • Metabolism by hepatic CYP450
    (affected by drugs that induce/inhibit hepatic metabolism)
  • Acid peptic disease (duodenal and gastric)
  • Control of Zollinger-Allison syndrome (gastrin-secreting
    neuroendocrine tumor)
  • Gastroesophageal reflux disease (GERD)
  • Stress ulcers, mucosal erosion, gastric hemorrhage in
    ICU patients (given IV)
  • Not 1st-line agent in the reduction of gastric acidity! (initial approach is based on treatment with PPI’s)
  • Side effects: cimetidine (but not other agents) is a weak antiandrogenic agent and a potent P450 enzyme inhibitor
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22
Q

Eicosanoid agonists

A 
Misoprostol
Alprostadil
Dinoprostone
Carboprost
Latanoprost
Epoprostenol
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23
Q

Misoprostol

Study These Flashcards
A

Eicosanoid agonists

PGE1 analogue

  • Oral
  • Abortifacient, in combination with mifepristone (progesterone antagonist)
  • effective up to 60 days into uterine pregnancy (extrauterine abortion is induced with methotrexate)
  • GI cytoprotective role → prophylaxis and treatment of NSAID’s-induced ulcers and erosions
24
Q

Alprostadil

Study These Flashcards
A

Eicosanoid agonists

PGE1 analogue

  • Parenteral
  • Male impotence (injection into corpus cavernosum)
  • Maintain patency of the ductus arteriosus in infants with transposition of the great vessels (until surgical
    correction can be undertaken)
25
Dinoprostone
Eicosanoid agonists PGE2 analogue - Vaginal gel - Abortifacient (2nd trimester) - Cervical ripening → soften the cervix at term before induction of labor with oxytocin
26
Carboprost
Eicosanoid agonists PGF2α analogue - Parenteral - Control of postpartum uterine bleeding - Abortifacient (2nd trimester)
27
Latanoprost
Eicosanoid agonists PGF2α analogue - Topical - Glaucoma (intraocular pressure ↓)
28
Epoprostenol
Eicosanoid agonists PGI2 analogue - Parenteral - Pulmonary hypertension - Antiplatelet agent in extracorporeal dialysis
29
Eicosanoid antagonists
Corticosteroids: PLA2 inhibitors, COX inhibitors (non-selective) ``` NSAID's: COX inhibitors (non-selective) ``` Celecoxib: COX-2 selective inhibitor Zileuton: LOX selective inhibitor Zafirlukast, Montelukast: LTD4 receptor antagonists
30
Drugs acting on the gastrointestinal and genitourinary tracts
Smooth muscle contraction: 1. Bethanechol 2. Neostigmine Smooth muscle relaxation: 1. Butyl- scopolamine 2. Solifenacin 3. Oxybutynin 4. Tolterodine 5. Papaverine 6. Drotaverine
31
Bethanechol
SM contraction Muscarinic agonist (selective) (direct-acting sympathomimetic) - Oral - Duration of action 30 min' - 2 h' - Poor lipid solubility (no CNS effects) - Non-obstructive ileus (postoperative) - Urinary retention
32
Neostigmine
SM contraction Acetylcholine-esterase inhibitor (indirect-acting sympathomimetic) - Oral - Duration of action 2-4 h' - Quaternary amine – does not enter CNS - Non-obstructive ileus (postoperative) - Urinary retention
33
Butyl- scopolamine
Smooth muscle relaxation Cholinergic receptor blocker (non-selective) - Oral - No CNS effects - GI spasm - Management of abdominal pain and discomfort caused by GI cramps, menstrual cramps, biliary colic, renal colic
34
Solifenacin | Tolterodine
Smooth muscle relaxation Cholinergic receptor blockers (modest selectivity for M3) - Oral, transdermal patch - No CNS effects - Bladder spasm (post-operative, neurogenic) - overactive bladder - Urinary incontinence
35
Oxybutynin
Smooth muscle relaxation Cholinergic receptor blockers (modest selectivity for M3) - Oral, transdermal patch - No CNS effects - Bladder spasm (post-operative, neurogenic) - Urinary incontinence
36
Papaverine
Smooth muscle relaxation ``` Ca2+-channel blocker PDE inhibitor (non-selective) ``` - Opioid alkaloid derivative - Oral, parenteral - Gastrointestinal and genitourinary spasm Side effects: - Cardiac → negative ionotropic, arrhythmia, hypotension - Hepatotoxicity - GI irritation - Priapism
37
Drotaverine
Smooth muscle relaxation ``` Ca2+-channel blocker PDE inhibitor (non-selective) ``` - Opioid alkaloid derivative - Oral, parenteral - Used to enhance cervical dilation during childbirth
38
Drugs acting on the female reproductive system
Tocolytic drugs – Agents relaxing the pregnant uterus 1. Atosiban 2. Terbutaline 3. Mg2+-sulphate 4. Ethanol Agents relaxing the non-pregnant uterus 1. NSAID's - Ibuprofen - Naproxen Agents contracting the pregnant uterus 1. Oxytocin (Pitocin) 2. Ergotamine 3. Ergonovine 4. Misoprostol 5. Dinoprostone 6. Carboprost
39
Atosiban
Tocolytic drugs – Agents relaxing the pregnant uterus Oxytocin receptor antagonist - IV - Not approved in all countries - Tocolytic agent (suppress preterm labor) *effective from gestational week 24 Side effects: - Increased rates of infant death
40
Terbutaline
Tocolytic drugs – Agents relaxing the pregnant uterus β2-selective agonist (SABA) - Aerosol inhalation, parenteral, oral - Rapid onset of action - Tocolytic agent * effective from gestational week 16 Side effects: - Cardiac stimulant effect with arrhythmias (may affect both mother and fetus)
41
Mg2+-sulphate
Tocolytic drugs – Agents relaxing the pregnant uterus IV - Tocolytic agent - Seizure prevention in preeclampsia/eclampsia - Protective role on fetal brain Side effects: - Maternal → flushing, lethargy, headache, weakness, pulmonary edema, cardiac arrest - Neonatal → hypotension, respiratory depression
42
Ethanol
Tocolytic drugs – Agents relaxing the pregnant uterus IV - Tocolytic agent
43
NSAID's - Ibuprofen - Naproxen
Agents relaxing the non-pregnant uterus COX inhibition → reduced PGF2α → uterine contraction ↓ - Oral - Dysmenorrhea (menstrual cramps) - Contraindicated during pregnancy (PGE2 maintains patent ductus arteriosus)
44
Oxytocin (Pitocin)
▪ Agents contracting the pregnant uterus Oxytocin receptor agonist (induces uterine contraction) Oxytocin Receptor (OTR): G-protein coupled receptor family, Gq. - Induces uterine contractions (frequency and intensity). - Sensitivity only in the peripartum period. Indication: labor initiation,  pain intensity, postpartum haemorrhage, promote milk release. - formul.: inj. (i.v., i.m.), nasal spray. - Short duration (t1/2 few min) - IV, intranasal - Induction and augmentation of labor - Control of postpartum uterine hemorrhage (high doses) - Induction of lactation (intranasal preparation) Side effects: - Fetal distress - Placental abruption - Uterine rupture
45
Ergotamine | Ergonovine
▪ Agents contracting the pregnant uterus Induces vasoconstriction and uterine contraction - Ergot alkaloid derivatives - Parenteral - Control of postpartum uterine hemorrhage * must not be given before delivery of the placenta
46
Misoprostol
▪ Agents contracting the pregnant uterus PGE1 analogue - Oral - Abortifacient, in combination with mifepristone (progesterone antagonist) *effective up to 60 days into pregnancy
47
Dinoprostone
▪ Agents contracting the pregnant uterus PGE2 analogue - Vaginal gel - Abortifacient (2nd trimester)
48
Carboprost
▪ Agents contracting the pregnant uterus PGF2α analogue - Parenteral - Control of postpartum uterine hemorrhage - Abortifacient (2nd trimester)
49
Drugs acting on the male reproductive system
Agents acting on the male reproductive system Tamsulosin Sildenafil
50
Tamsulosin
'Uroselective' α-blocker (inhibits α1A sparing α1B receptors→ no hypotension) - Oral - Hypertension - Benign prostatic hyperplasia (BPH) → relax the muscle of the prostate and bladder neck, which allows urine to flow more easily
51
Sildenafil
PDE-5 inhibitor - Oral - Erectile dysfunction - Pulmonary hypertension Side effects: - Severe hypotension in combination with nitrates - Priapism (prolonged erection) - Blue-tinted vision (via inhibition of PDE-6 in retina)
52
Treatment of glaucoma
Pilocarpine: Ciliary muscle contraction  (up) aqueous humors outflow  decrease in intraocular pressure
53
Ergotamine
Affects several receptors (5HT-, D-, α-adrenergic Receptors). Potent uterine contrictor  narrows the blood vessels running through myometrium reduces bleeding. Use: post-partum bleeding, promote involution. Side effects: increased blood pressure, reflex bradycardia. Migraine therapy (constriction of the intracranial extracerebral blood vessels) (ergotamine and dihydroergotamine)
54
Endogenous smooth muscle relaxants
Ach Amines: adrenaline (ß2 arteries and bronchi) histamine (reduces peripheral vascular resistance) ``` Nitric oxide (NO): relaxation of the smooth muscle in the corpora cavernous—the initiating factor in penile erection. ``` ATP and its derivatives Neuropeptides (VIP, PACAP, Bradykinin
55
Anticholinergic agents: | Contraindications and side effects
Contraindications - Partial or complete GI obstruction. - Paralytic ileus. - Urinary retention. - Narrow angle glaucoma. - Gastric retention. - Myasthenia gravis. - Obstructive uropathy. Side agents effects: Dry mouth Constipation Blurred vision

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