AUTOCOID & AUTOCOID ANTAGONIST

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 Autocoid

 Endogeenous ccompound act on the Tissue from where they formed Histamine, Prostglandin, Serotonin

Prostaglandinns Mifepristone, Misoprostol

H1-Anti-Histamine(First Generation) Chlorpheniramine, Cyclizine, Diphenhydramine, Dimenhydrinate, Doxepin, Doxylamine, Hdroxyzine, Meclizine, Promethazine

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H1-Anti-Histamine(2nd Generation) Acrivastine, Cetrizine, Desloratadine, Fexofenadine, Loratadine


Drug for Migraine Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan


Histamine

 Chemical messenger, generated in Mast cell...No therapeutic effect but Anti-Histamine have Therapeutic effect...

Location

Found in Lung, Skin, GIT...Histamine found in Mast cell, Basophil, Insect sting, Venom

Synthesis

Histidine→Histamine by Decarboxylation...Stored as Histamine complex with Heparin (PolySulfated anion)...Histamine inactivated by Amine oxidase

Release

 By Cold, Bacterial toxin, Bee Sting, Trauma, Allergies, Anaphylaxis

MOA

H1, H2, H3, H4 receptors...H1, H2 widely expressed...H1 involved in ↑NO, Vasodilation, ↑IP3,DAG,↑Ca++...Smooth muscle contraction

H2 involved in ACID release from Parietal cells

H1-ANTI-HISTAMINE

Block receptor mediatedrsponse of Histamine...

don‟t effect its formation(Cromolyn block Histamine release from Mast cell)

T.E

DOC in Urticaria & Allergic Rhinitis...not used in Asthma...

Diphenhydraine

Dimenhydrinate, Cyclizine, Meclizine, Hydroxazine used in MOTION SICKNESS

Diphenhydramine, Doxylamine used as SOMNIFACIENT in Insomnia

2nd Generation

not cross B.B.B sodo no cause SEDATION as 1st Generation

S.E

Sedation, Dry mouth ...Overdose; Coma, Cardio-Respiratory collapse

DRUGS FOR MIGRAINE

Migraine

Pulsatile, throbbing pain

Cluster-Headache

 Sharp, steady pain

Tension type headache

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 Dull pain, persistent Tightening feeling in head

Types of Migraine

Common Headache

without AURA, Severe, Unilateral,

Pulsating Headache lasts 2-72hr...aggaravated by Physical activity...followed by Nausea, Vomiting, Photophobia, Phonophobia

Classic Migraine

With AURA, with Neurological symptoms i.e Visual, Speeech,

Motor disturbance, lasts 20-40min

Biologic Basis of Migraine

Reduced Blood flow to Cerebral Hemisphere...

Extra/Intra-Cranial Dilation, Release of Substance P

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Symptomatic treatment

5-HTD1 Agonist (Triptan, Dihydroergotamine)

Triptans

Nausea with Dihydroergotamine less with Triptan...

Zolmitriptan oraly & nasal spray, short half life...Frovatriptan longest half life

S.E

 Pain & Pressure sensation in Chest, Jaw, Throat, Neck...Contra in CHF

Dihydroergotamine IV...nausea

Prophylaxis Propranolol DOC for prophylaxis ...Nodalol also used

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