Autacoids Flashcards by Mark Agustin

(BESH)

Bradykinin
Eicosanoids
Serotonin
Histamine

Autacoids

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Receptors -> Effects

H1=
H2 =
H3 =
H4 =

H1= allergy
H2 = acidity; allergy
H3 = inhibitory
H4 = inflammation

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What Receptors is stated below:

▪️ Blood vessels: vasodilation
▪️ Bronchi: bronchoconstriction
▪️ Sensory nerrve endings: pain
▪️ Endothelial Cells: contraction
▪️ CNS (brain): alertness/weakfulness

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What Receptors is stated below:

▪️Acidity: parietal cells
▪️Allergy: mast cells & basophils
▪️peaks at night

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What Receptors is stated below:

▪️CNS (pre-synaptic)-inhibitory effect
▪️(-) further release of histamine
▪️↓ histamine

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What Receptors is stated below:

▪️Inflammation (neutrophils)
▪️= chemotaxis

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Histamine Agonist

▪️H1 agonist, H3 antagonist
▪️Mgt. of endolymph (presence of fluid in inner ear) asssociated with vertigo

Betahistine (Serc)

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Histamine Agonist

▪️investigational drug

Impromidine

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What Generation of Antihistamine is stated below:

▪️Sedating Antihistamine
▪️lipophilic-can pass through BBB
▪️Majority (6)

First Generation/Classical Antihistamine

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What are the 6 class/types of First Gen. Antihistamine

Ethanolamines
Ethylenediamines
Piperazines
Alkylamines
Phenothiazine
Piperidine

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What type of First Gen. Antihistamine is stated below:

▪️most sedating
▪️most effective

Ethanolamines

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What drug is stated below (under Ethanolamines)

▪️BN: Benadryl
▪️Used for Dystonia (clinical prep. of EPS), Torti coilis (twisting of the neck)
▪️antimuscarinic effect

Diphenhydramine

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What drug is stated below (under Ethanolamines)

▪️ salt form of Diphenhydramine

Dimenhydrinate

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What drug is stated below (under Ethanolamines)

▪️BN: Unisom tablet
▪️sleeping aid
▪️most sedating

Doxylamine

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First Gen. Antihistamine

▪️Pyrilamine
▪️Tripelennamine
- causes GI upset, mild sedation

Ethylenediamines

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1st Gen Antihistamine

Drugs under Piperazines

Meclizine (Bonamine)
Cyclizine
Hydroxyzine (Iterax) - prodrug; active form is Cetirizine

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1st Gen Antihistamine (under Piperazines)

▪️tx. of motion sickness

Meclizine (Bonamine), Cyclizine

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1st Gen Antihistamine (under Phenothiazine)

▪️anesthetic agent: to induce pre-opera sedation

Promethazine (Phenergan)

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1st Gen Antihistamine (under Piperidine)

▪️5-HT Antagonist - blocks 5-HT1 & 5-HT2
▪️Mgt. of Serotonin Syndrome (muscle rigidity, hyperthermia)

Cyproheptadine

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What class/type of Second Generation Antihistamine is considered as LESS SEDATING

Piperazines

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What class/type of Second Generation Antihistamine is considered as NON SEDATING

Piperidine

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2nd Gen. Antihistamine

What drugs is under Piperazines

Cetirizine (Virlix, Zyrtec, Alnix)
Levocetirizine (Allerzet)

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BN: of Levocetirizine with Montelukast

Zyrkast
Co-Altria

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BN of Levocetirizine

Allerzet

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BN of Cetirizine

Virlix Zyrtex Alnix

2nd Gen. Antihistamine What drugs is under Piperidines

Loratadine (Claritin, Allerta) Desloratadine (Aerius) Fexofenadine (Telfast) from Terfenadine [cardiotoxic)

What are the Newer Drugs for 2nd Gen. Antihistamine

Bilastine (Bilaxten) Ebastine + Betamethasone (Co-Aleva)

What are the class/type of 2nd Gen. Antihistamine are advice to take for Pilots, Drivers, and Machine Operators

Piperidines - Loratadine, Desloratadine, Fexofenadine

What type of generation antihistamines are allowed to be used by pilots?

Second Generation Antihistamine

What type of generation antihistamine is more potent

First Generation Antihistamine

What are the drugs under H2 Antihistamine Antagonist (4-CFNR-idine)

1. Cimetidine (Tagamet) 2. Famotidine (H2-Bloc) 3. Nizatidine (Axid) 4. Ranitidine (Zantac)

What drug or class type is stated below: ▪️Mgt. of Acid Peptic Disease ▪️Mgt. of Acute GI Ulcer Bleeding ▪️Adjuncts -> Allergy

H2 Antihistamine (Cimetidine, Famotidine, Nizatidine, Ranitidine)

Most potent H2 Antihistamine

Famotidine

Least potent H2 Antihistamine

Cimetidine

Serotonin Receptors 5-HT1 & 5-HT4

Agonist

Serotonin Receptors 5-HT2 & 5-HT3

Antagonist

What Receptors of Serotonin is stated below: ▪️Location: Presynaptic (CNS/Brain) ▪️(-) further release of 5-HT

5-HT1a

What is the chemical name of Serotonin

5-hydroxytryptamine (5-HT)

What Receptors of Serotonin is stated below: ▪️Location: Cerebral BV ▪️Cerebral Vasoconstriction = antimigraine

5-HT1b/1d

What Receptors of Serotonin is stated below: ▪️Location: smooth muscles (uterus, cerebral BV, bronchi) ▪️Contraction, Oxytosis, Vasoconstriction, Bronchoconstriction, Aggregation, Peristalsis

5-HT2a/2b

What Receptors of Serotonin is stated below: ▪️Location: Chemoreceptor Trigger Zone (CTZ) ▪️Emesis, Vomiting Center ▪️ ▪️

5-HT3

What Receptors of Serotonin is stated below: ▪️Location: GIT ▪️Peristalsis

5-HT4

[ 5-HT1a ] What drug is stated below: ▪️Partial Agonist ▪️Use: Anxiolytic

Buspirone

[ 5-HT1b/1d ] What drug is stated below: ▪️Full Agonist ▪️Use: Antimigraine ▪️-triptans

Sumatriptan Naratriptan Zolmitriptan

[ 5-HT4] What drug is stated below: ▪️Partial Agonist ▪️Use: Mgt. of irritable bowel syndrome (constipation)

Cisapride Tegaserod

[ 5-HT4 ] What drug is stated below: ▪️Full Agonist ▪️Use: Mgt. of irritable bowel syndrome (constipation)

Prucalopride

What drug is stated below: ▪️Receptor: 5HT1&2 ▪️Use: Serotonin Syndrome

Cyproheptadine

[ 5-HT3 ] What drug is stated below: ▪️Antagonist ▪️Use: Antiemetics (cancer chemotherapy) ▪️-setron

Ondasetron Granisetron Palonosetron

[ 5-HT2a/2b ] What drug is stated below: ▪️Antagonist ▪️Use: Antihypertensive, Prevents platelet aggregation

Ketanserin Ritanserin

What drug is under 5-HT3 but not used as antiemetic instead it was used for management of irritable bowel syndrome (IBS) diarrhea

Alosetron

From Claviceps purpurea- target a, DA, 5-HT2 (mixed action)

Ergots

What drugs of Ergots Agonist is stated below: ▪️vasoselective ▪️antimigraine

Ergotamine

What drugs of Ergots Agonist is stated below: ▪️uteroselective ▪️tx: post-partum bleeding ▪️antimigraine

Ergonovine

What drugs of Ergots Antagonist is stated below: ▪️ prophylaxis of migraine headaches

Methysergide

What is stated below: ▪️Products of eicosanoic acid metabolism ▪️Polyunsaturated Fatty acids (PUFA) Major: Arachidonic acid ▪️Enzymes: COX, 5-LOX

Eicosanoids

What type of Eicosanoid is stated below: ▪️Blood Vessels - Vasoconstriction: TXA2 - Vasodilation: PGI2

Vasoconstriction: TXA2 Vasodilation: PGI2

What type of Eicosanoid is stated below: ▪️Injured Tissues - Inflammation

PGE2 (major inflammatory) PGI2 LTB4 (chemotaxis)

What type of Eicosanoid is stated below: ▪️Bronchi - Bronchoconstriction - Bronchodilation

Bronchoconstriction: LTC4, LTD4 Bronchodilation: PGE series

What type of Eicosanoid is stated below: ▪️Uterus - contraction - oxytocic, dysmenorrhea

PGE series, PGF

What type of Eicosanoid is stated below: ▪️Platelets - Aggregation (clot): - (-) aggregation:

Aggregation (clot): TXA2 (-) aggregation (bleeding): PGI2

What type of Eicosanoid is stated below: ▪️Eyes - Reduction IOP

Reduction IOP: PGF2a

What Drugs of Prostaglandin Analogues [MEDAL]

Misoprostol Epoprostenol Dinoprostone Alprostadil Latanoprost

What Drug of Prostaglandin Analogues is stated below: ▪️BN: Cytotec ▪️PGE1 ▪️Effect: Cytoprotection ▪️Use: Tx. of NSAIDs- induced ulcer, abortifacient

Misoprostol

What Drug of Prostaglandin Analogues is stated below: ▪️PGI2 ▪️Effect: Vasodilation (systemic) ▪️Use: Mgt. of 1° Pulmonary HTN

Epoprestenol

What Drug of Prostaglandin Analogues is stated below: ▪️PGE2 ▪️Effect: cervical ripening ▪️Use: Therapeutic Abortion-FDA approved abortifacient

Dinoprostone

What Drug of Prostaglandin Analogues is stated below: ▪️PGE1 ▪️Effect: Vasodilation (local) ▪️Use: Tx. of erectile dysfunction

Alprostadil

What drug is use for closure of Ductus Arteriosus

Indomethacin

What Drug of Prostaglandin Analogues is stated below: ▪️BN: Xalatan ▪️PGF2a ▪️Effect: Decrease IOP ▪️Use: Antiglaucoma

Latanoprost (also: Carboprost)