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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

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

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

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
Q

Dinoprostone

A

Eicosanoid agonists

PGE2 analogue

  • Vaginal gel
  • Abortifacient (2nd trimester)
  • Cervical ripening → soften the cervix at term before
    induction of labor with oxytocin
26
Q

Carboprost

A

Eicosanoid agonists

PGF2α analogue

  • Parenteral
  • Control of postpartum uterine bleeding
  • Abortifacient (2nd trimester)
27
Q

Latanoprost

A

Eicosanoid agonists

PGF2α analogue

  • Topical
  • Glaucoma (intraocular pressure ↓)
28
Q

Epoprostenol

A

Eicosanoid agonists

PGI2 analogue

  • Parenteral
  • Pulmonary hypertension
  • Antiplatelet agent in extracorporeal dialysis
29
Q

Eicosanoid antagonists

A

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
Q

Drugs acting on the gastrointestinal and genitourinary tracts

A

Smooth muscle contraction:

  1. Bethanechol
  2. Neostigmine

Smooth muscle relaxation:

  1. Butyl- scopolamine
  2. Solifenacin
  3. Oxybutynin
  4. Tolterodine
  5. Papaverine
  6. Drotaverine
31
Q

Bethanechol

A

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
Q

Neostigmine

A

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
Q

Butyl- scopolamine

A

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
Q

Solifenacin

Tolterodine

A

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
Q

Oxybutynin

A

Smooth muscle relaxation

Cholinergic receptor blockers (modest selectivity for M3)

  • Oral, transdermal patch
  • No CNS effects
  • Bladder spasm (post-operative, neurogenic)
  • Urinary incontinence
36
Q

Papaverine

A

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
Q

Drotaverine

A

Smooth muscle relaxation

Ca2+-channel blocker
PDE inhibitor (non-selective)
  • Opioid alkaloid derivative
  • Oral, parenteral
  • Used to enhance cervical dilation during childbirth
38
Q

Drugs acting on the female reproductive system

A

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
Q

Atosiban

A

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
Q

Terbutaline

A

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
Q

Mg2+-sulphate

A

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
Q

Ethanol

A

Tocolytic drugs – Agents relaxing the pregnant uterus

IV
- Tocolytic agent

43
Q

NSAID’s

  • Ibuprofen
  • Naproxen
A

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
Q

Oxytocin (Pitocin)

A

▪ 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
Q

Ergotamine

Ergonovine

A

▪ 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
Q

Misoprostol

A

▪ Agents contracting the pregnant uterus

PGE1 analogue

  • Oral
  • Abortifacient, in
    combination with mifepristone (progesterone antagonist)
    *effective up to 60 days into pregnancy
47
Q

Dinoprostone

A

▪ Agents contracting the pregnant uterus

PGE2 analogue

  • Vaginal gel
  • Abortifacient (2nd trimester)
48
Q

Carboprost

A

▪ Agents contracting the pregnant uterus

PGF2α analogue

  • Parenteral
  • Control of postpartum uterine hemorrhage
  • Abortifacient (2nd trimester)
49
Q

Drugs acting on the male reproductive system

A

Agents acting on the male reproductive system

Tamsulosin

Sildenafil

50
Q

Tamsulosin

A

‘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
Q

Sildenafil

A

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
Q

Treatment of glaucoma

A

Pilocarpine: Ciliary muscle contraction  (up) aqueous humors outflow  decrease in intraocular pressure

53
Q

Ergotamine

A

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
Q

Endogenous smooth muscle relaxants

A

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
Q

Anticholinergic agents:

Contraindications and side effects

A

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

immunopharmacology (10 decks)

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