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Pharmacology - Block 2 - Part 7

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davidwurbel7's version from 2016-07-04 01:18

Histamine, Serotonin & Ergot alkaloids, Eicosanoids & Nitric Oxide

Question Answer
Histamine receptor found in the blood vessels and bronchial smooth muscleH1
This histamine receptor is a Gq coupled receptorH1
Histamine receptor found in the stomachH2
This histamine receptor is a Gs coupled receptorH2
Histamine is found in mast cells, basophils, cells of the epidermis, cells in the gastric mucosa, neurons, cells of rapidly growing tissues and also hereChromaffin Cells
The mechanism of action inhibits both antigen- and exercise-induced asthma, and chronic use slightly reduces the overall level of bronchial reactivity. The cellular mechanism alteration in the function of delayed chloride channels in the cell membrane that inhibits cellular activation in eosinophils & specific mast cells subtypes found in the lung. Indications - Prophylaxis for inhibiting asthma caused by allergens or exerciseCromolyn Sodium, Nedocromil
These drug work as mast cell stabilizers and degranulation inhibitorsCromolyn Sodium, Nedocromil
Diphenhydramine, Chlorpheniramine, Promethazine are examples of this class of drugFirst Generation H1 Antihistamines
This class of antihistamines has the following additional effects peripheral antimuscarinic actions, Central antimuscarinic actions (which leads to its use in treating drug induced EPS) and Adrenoceptor‑blocking actions (some compounds)First Generation H1 Antihistamines
This class of antihistamines has a sedative (cause drowsiness) effectFirst Generation H1 Antihistamines
Loratidine, Fexofenadine, Cetirizine, Azelastin are examples of this class of drugSecond Generation H1 Antihistamines
This class of antihistamines does not have a sedative (cause drowsiness) effectSecond Generation H1 Antihistamines
The mechanism of action is a competitive H1 receptor antagonist. Indications - Antihistaminic - For allergic conjunctivitis allergic skin manifestations of urticaria and angioedema. Motion sickness - act by blocking muscarinic receptors in the vestibular & vomiting centers. Antiparkinsonism - For antipsychotic drug induced Extrapyramidal Symptoms (EPS). Sedation - used as a mild sedativeFirst Generation H1 Blockers
Adverse effects - Marked Sedation and motor incoordination. Antimuscarinic side effect - dry mouth, blurring of vision, urinary hesitancy. Postural hypotension – due to alpha R blocking action. Major drug interactions - has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc)First Generation H1 Blockers
The Mechanism of Action selective peripheral H1-receptor antagonist activity. Indications - seasonal allergic rhinitis in adults and children 6 years of age and older. Chronic idiopathic urticaria in adults and children 6 years of age and older. Side Effects - less lipid soluble, and hence have little or no sedative and far fewer autonomic effects. They have no effect on muscarinic receptors and alpha adrenergic receptors. Drug Interaction - may cause tachycardia, arrhythmias (after high doses)Second Generation H1 Blockers
Terfenadine and astemizole, two second-generation agents, can cause this when given at high doses or with CYP inhibitors (like erythromycin and antifungal azoles)Polymorphic Ventricular Tachycardia (torsades de pointes)
Fexofenadine is the metabolite of thisTerfenadine
Fexofenadine is better than terfenadine due to this propertyNon-Cardiogenic Effect
The side effects of dry mouth, blurring of vision, urinary hesitancy is due to this effect of H1 blockersAntimuscarinic Side Effect
The seide effect of postural hypotension is due to this effect of H1 blockersAlpha Receptor Blocking
Serotonin is metabolized by MAO to form this5 - Hydroxyindoleacetic Acid (5HIAA)
Marker of carcinoid syndrome5 - Hydroxyindoleacetic Acid (5HIAA)
Serotonin receptor found in the raphe nuclei5HT1A (Generalized Anxiety)
Serotonin receptor found in the cranial blood vessels5HT1D (Headache)
Serotonin receptor found in the platelets, smooth muscle and CNS5HT2A
Serotonin receptor found in the enteric nerves and area postrema (vomit center)5HT3
Serotonin receptor found in the myenteric neurons, smooth muscle and CNS5HT4
This serotonin receptor is a Gi coupled receptor5HT1
This serotonin receptor is a Na+/K+ ion channel receptor5HT3
5 HT1B/D agonist. Used for acute migraine attackSumatriptan
5HT1A agonist. Used as an anxiolytic drugBuspirone
5HT4 agonist. Used in irritable bowel syndrome when associated with constipationTegaserod
Antiemetic used to control of vomiting associated with chemotherapyOndansetron
Antiemetic used in irritable bowel syndrome with diarrheaAlosetron
LSD & Bromocriptine, pergolide are ergot alkaloids acting hereCNS
Ergonovine & Ergotamine are ergot alkaloids as well as misoprostol acting hereUterus
Ergotamine is an ergot alkaloids acting hereBlood Vessels
Ergonovine and Ergotamine are ergot alkaloids as well as misoprostol that are used for thisPost Partum Hemorrhage
These drugs can be used to treat post partum hemorrhageErgonovine, Ergotamine and Misoprostol
Bromocriptine, pergolide are ergot alkaloids that are used for thisHyperprolactinemia
These drugs can be used to treat hyperprolactinemiaBromocriptine and Pergolide
Bromocriptine is an ergot alkaloid that can be used to treatParkinson’s disease
This drug can be used to treat Parkinson's diseaseBromocriptine
Ergotamine is an ergot alkaloid that can be used to treatAcute attack of migraine
These drugs can be used to treat acute attack of moderate- severe migraineSumatriptan and Ergotamine
Sumatriptan, Rizatriptan, Eletriptan , Almotriptan are examples of this class of drugsTriptans
The mechanism of action - Selective Serotonin (5-HT1B/1D) agonists. Activation of 5HT1B or 5-HT1D receptors inhibits the activation of the trigeminal nerve and this effect inhibits meningeal vasodilation. By this mechanism these drugs produce meningeal vasoconstriction. Indications - Acute treatment of migraineTriptans
Contraindications - cardiac ischemia, cerebrovascular, or peripheral vascular disease. Side Effects include coronary artery vasospasm, hypertensive episodesTriptans
The mechanism of action - Partial agonists at alpha-adrenergic receptors in blood vessels, resulting in vasoconstriction. Indications - acute treatment of migraine headaches. Contraindications - pregnancy vascular disease (e.g. coronary artery disease, hypertension) psychosis. Side Effects - overdosage produces a characteristic poisoning called ergotism or “St. Anthony’s fire”: prolonged vasospasm resulting in gangrene and amputations; hallucinations and dementia; and abortionsErgotamine
The mechanism of action - 5-HT1D agonist which causes vasoconstriction of intracranial blood vessels; stimulation of 5-HT1D receptors on sensory nerve endings in the trigeminal system, resulting in an inhibition of release of pro-inflammatory neuropeptides. Indications - acute treatment of migraine headaches. Contraindications - pregnancy vascular disease (e.g. coronary artery disease, hypertension) psychosis. Side Effects - overdosage produces a characteristic poisoning called ergotism or “St. Anthony’s fire”: prolonged vasospasm resulting in gangrene and amputations; hallucinations and dementia; and abortionsDihydroergotamine
An overdose of Ergots produce prolonged vasospasm resulting in gangrene and amputations; convulsions, hallucinations and dementia; abortions. These set of symptoms are known asSt. Anthony's Fire
Mechanism of Action - β-1 receptor blockers without intrinsic sympathomimetic activity. Reduces the neuronal firing rate of noradrenergic neurons of the locus coeruleus regulate the firing rate of periaqueductal grey matter neurons via a GABA-mediated actionPropranolol
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Question Answer
Prostaglandin that keeps the Ductus arteriosus (DA) open in fetusPGE
Patent Ductus arteriosus in which no cyanosis is seenIndomethacin
Cyanotic heart diseases in which the ductus arteriosus must be kept openAlprostadil (PGE)
Misoprostol (PGE1) with mifepristone (antiprogestin) is used for thisAbortion
Dinoprostone (PGE2) and Carboprost (PGF2α) can be used for thisCervical Ripening
This prostaglandin is used in treatment of NSAID –induced peptic ulcersMisoprostol
This class of drugs is used for dysmenorrhea but to inhibition of the synthesis of prostaglandinsNSAIDs
Synthetic PGE1 delivered into corpus cavernousum as suppository induces erection in dysfunctional malesAlprostadil (PGE)
In Glaucoma, increases the out flow from anterior chamber and decreases the intraoccular pressureLatanoprost (PGF2α)
This drug is use in pulmonary hypertension and is a platelet stabilizer and vasodilatorEpoprostenol
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Question Answer
Alprostadil prostaglandin classPGE
Misoprostol prostaglandin classPGE
Carboprost prostaglandin classPGF
Dinoprostone prostaglandin classPGF
Epoprostenol prostaglandin classPGI
Latanoprost prostaglandin classPGF
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Question Answer
Alprostadil treatsErectile Dysfunction
Misoprostol treatsPeptic Ulcer
Carboprost treatsCervical Ripping
Dinoprostone treatsCervical Ripping
Epoprostenol treatsPulmonary Hypertension
Latanoprost treatsGlaucoma
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Question Answer
Zileuton5-lipoxygenase enzyme inhibitors
Zafirlukast and monteleukastLeukotriene Receptor Antagonist
Zileuton, Zafirlukast and monteleukast are used for the treatment of thisBronchial Asthma
This drug selectively inhibits the predominant phosphodiesterase (type 5) expressed in the male corpus cavernosum which breaks down cGMPSildenafil
Contraindications include coadministration of a nitrate within 24 hours is likely to produce an exagerated hypotensive responseSildenafil
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