Autacoids Flashcards
(BESH)
Bradykinin
Eicosanoids
Serotonin
Histamine
Autacoids
Receptors -> Effects
H1=
H2 =
H3 =
H4 =
H1= allergy
H2 = acidity; allergy
H3 = inhibitory
H4 = inflammation
What Receptors is stated below:
▪️ Blood vessels: vasodilation
▪️ Bronchi: bronchoconstriction
▪️ Sensory nerrve endings: pain
▪️ Endothelial Cells: contraction
▪️ CNS (brain): alertness/weakfulness
H1
What Receptors is stated below:
▪️Acidity: parietal cells
▪️Allergy: mast cells & basophils
▪️peaks at night
H2
What Receptors is stated below:
▪️CNS (pre-synaptic)-inhibitory effect
▪️(-) further release of histamine
▪️↓ histamine
H3
What Receptors is stated below:
▪️Inflammation (neutrophils)
▪️= chemotaxis
H4
Histamine Agonist
▪️H1 agonist, H3 antagonist
▪️Mgt. of endolymph (presence of fluid in inner ear) asssociated with vertigo
Betahistine (Serc)
Histamine Agonist
▪️investigational drug
Impromidine
What Generation of Antihistamine is stated below:
▪️Sedating Antihistamine
▪️lipophilic-can pass through BBB
▪️Majority (6)
First Generation/Classical Antihistamine
What are the 6 class/types of First Gen. Antihistamine
- Ethanolamines
- Ethylenediamines
- Piperazines
- Alkylamines
- Phenothiazine
- Piperidine
What type of First Gen. Antihistamine is stated below:
▪️most sedating
▪️most effective
Ethanolamines
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
What drug is stated below (under Ethanolamines)
▪️ salt form of Diphenhydramine
Dimenhydrinate
What drug is stated below (under Ethanolamines)
▪️BN: Unisom tablet
▪️sleeping aid
▪️most sedating
Doxylamine
First Gen. Antihistamine
▪️Pyrilamine
▪️Tripelennamine
- causes GI upset, mild sedation
Ethylenediamines
1st Gen Antihistamine
Drugs under Piperazines
Meclizine (Bonamine)
Cyclizine
Hydroxyzine (Iterax) - prodrug; active form is Cetirizine
1st Gen Antihistamine (under Piperazines)
▪️tx. of motion sickness
Meclizine (Bonamine), Cyclizine
1st Gen Antihistamine (under Phenothiazine)
▪️anesthetic agent: to induce pre-opera sedation
Promethazine (Phenergan)
1st Gen Antihistamine (under Piperidine)
▪️5-HT Antagonist - blocks 5-HT1 & 5-HT2
▪️Mgt. of Serotonin Syndrome (muscle rigidity, hyperthermia)
Cyproheptadine
What class/type of Second Generation Antihistamine is considered as LESS SEDATING
Piperazines
What class/type of Second Generation Antihistamine is considered as NON SEDATING
Piperidine
2nd Gen. Antihistamine
What drugs is under Piperazines
Cetirizine (Virlix, Zyrtec, Alnix)
Levocetirizine (Allerzet)
BN: of Levocetirizine with Montelukast
Zyrkast
Co-Altria
BN of Levocetirizine
Allerzet
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)
- Cimetidine (Tagamet)
- Famotidine (H2-Bloc)
- Nizatidine (Axid)
- 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)