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M4: Pharmacology-Pharmacokinetics > Autacoids > Flashcards

Autacoids Flashcards

1
Q

(BESH)

Bradykinin
Eicosanoids
Serotonin
Histamine

A

Autacoids

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2
Q

Receptors -> Effects

H1=
H2 =
H3 =
H4 =

A

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

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3
Q

What Receptors is stated below:

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

A

H1

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4
Q

What Receptors is stated below:

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

A

H2

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5
Q

What Receptors is stated below:

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

A

H3

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6
Q

What Receptors is stated below:

▪️Inflammation (neutrophils)
▪️= chemotaxis

A

H4

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7
Q

Histamine Agonist

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

A

Betahistine (Serc)

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8
Q

Histamine Agonist

▪️investigational drug

A

Impromidine

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9
Q

What Generation of Antihistamine is stated below:

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

A

First Generation/Classical Antihistamine

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10
Q

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

A
  1. Ethanolamines
  2. Ethylenediamines
  3. Piperazines
  4. Alkylamines
  5. Phenothiazine
  6. Piperidine
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11
Q

What type of First Gen. Antihistamine is stated below:

▪️most sedating
▪️most effective

A

Ethanolamines

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12
Q

What drug is stated below (under Ethanolamines)

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

A

Diphenhydramine

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13
Q

What drug is stated below (under Ethanolamines)

▪️ salt form of Diphenhydramine

A

Dimenhydrinate

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14
Q

What drug is stated below (under Ethanolamines)

▪️BN: Unisom tablet
▪️sleeping aid
▪️most sedating

A

Doxylamine

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15
Q

First Gen. Antihistamine

▪️Pyrilamine
▪️Tripelennamine
- causes GI upset, mild sedation

A

Ethylenediamines

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16
Q

1st Gen Antihistamine

Drugs under Piperazines

A

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

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17
Q

1st Gen Antihistamine (under Piperazines)

▪️tx. of motion sickness

A

Meclizine (Bonamine), Cyclizine

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18
Q

1st Gen Antihistamine (under Phenothiazine)

▪️anesthetic agent: to induce pre-opera sedation

A

Promethazine (Phenergan)

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19
Q

1st Gen Antihistamine (under Piperidine)

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

A

Cyproheptadine

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20
Q

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

A

Piperazines

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21
Q

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

A

Piperidine

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22
Q

2nd Gen. Antihistamine

What drugs is under Piperazines

A

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

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23
Q

BN: of Levocetirizine with Montelukast

A

Zyrkast
Co-Altria

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24
Q

BN of Levocetirizine

A

Allerzet

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25
Q

BN of Cetirizine

A

Virlix
Zyrtex
Alnix

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26
Q

2nd Gen. Antihistamine

What drugs is under Piperidines

A

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

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27
Q

What are the Newer Drugs for 2nd Gen. Antihistamine

A

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

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28
Q

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

A

Piperidines - Loratadine, Desloratadine, Fexofenadine

29
Q

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

A

Second Generation Antihistamine

30
Q

What type of generation antihistamine is more potent

A

First Generation Antihistamine

31
Q

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

A
  1. Cimetidine (Tagamet)
  2. Famotidine (H2-Bloc)
  3. Nizatidine (Axid)
  4. Ranitidine (Zantac)
32
Q

What drug or class type is stated below:

▪️Mgt. of Acid Peptic Disease
▪️Mgt. of Acute GI Ulcer Bleeding
▪️Adjuncts -> Allergy

A

H2 Antihistamine (Cimetidine, Famotidine, Nizatidine, Ranitidine)

33
Q

Most potent H2 Antihistamine

A

Famotidine

34
Q

Least potent H2 Antihistamine

A

Cimetidine

35
Q

Serotonin Receptors

5-HT1 & 5-HT4

A

Agonist

36
Q

Serotonin Receptors

5-HT2 & 5-HT3

A

Antagonist

37
Q

What Receptors of Serotonin is stated below:

▪️Location: Presynaptic (CNS/Brain)
▪️(-) further release of 5-HT

A

5-HT1a

38
Q

What is the chemical name of Serotonin

A

5-hydroxytryptamine (5-HT)

39
Q

What Receptors of Serotonin is stated below:

▪️Location: Cerebral BV
▪️Cerebral Vasoconstriction = antimigraine

A

5-HT1b/1d

40
Q

What Receptors of Serotonin is stated below:

▪️Location: smooth muscles (uterus, cerebral BV, bronchi)
▪️Contraction, Oxytosis, Vasoconstriction, Bronchoconstriction, Aggregation, Peristalsis

A

5-HT2a/2b

41
Q

What Receptors of Serotonin is stated below:

▪️Location: Chemoreceptor Trigger Zone (CTZ)
▪️Emesis, Vomiting Center
▪️
▪️

A

5-HT3

42
Q

What Receptors of Serotonin is stated below:

▪️Location: GIT
▪️Peristalsis

A

5-HT4

43
Q

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

A

Buspirone

44
Q

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

A

Sumatriptan
Naratriptan
Zolmitriptan

45
Q

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

A

Cisapride
Tegaserod

46
Q

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

A

Prucalopride

47
Q

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

A

Cyproheptadine

48
Q

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

A

Ondasetron
Granisetron
Palonosetron

49
Q

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

A

Ketanserin
Ritanserin

50
Q

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

A

Alosetron

51
Q

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

A

Ergots

52
Q

What drugs of Ergots Agonist is stated below:

▪️vasoselective
▪️antimigraine

A

Ergotamine

53
Q

What drugs of Ergots Agonist is stated below:

▪️uteroselective
▪️tx: post-partum bleeding
▪️antimigraine

A

Ergonovine

54
Q

What drugs of Ergots Antagonist is stated below:

▪️ prophylaxis of migraine headaches

A

Methysergide

55
Q

What is stated below:

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

A

Eicosanoids

56
Q

What type of Eicosanoid is stated below:

▪️Blood Vessels
- Vasoconstriction: TXA2
- Vasodilation: PGI2

A

Vasoconstriction: TXA2
Vasodilation: PGI2

57
Q

What type of Eicosanoid is stated below:

▪️Injured Tissues
- Inflammation

A

PGE2 (major inflammatory)
PGI2
LTB4 (chemotaxis)

58
Q

What type of Eicosanoid is stated below:

▪️Bronchi
- Bronchoconstriction
- Bronchodilation

A

Bronchoconstriction: LTC4, LTD4
Bronchodilation: PGE series

59
Q

What type of Eicosanoid is stated below:

▪️Uterus
- contraction
- oxytocic, dysmenorrhea

A

PGE series, PGF

60
Q

What type of Eicosanoid is stated below:

▪️Platelets
- Aggregation (clot):
- (-) aggregation:

A

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

61
Q

What type of Eicosanoid is stated below:

▪️Eyes
- Reduction IOP

A

Reduction IOP: PGF2a

62
Q

What Drugs of Prostaglandin Analogues [MEDAL]

A

Misoprostol
Epoprostenol
Dinoprostone
Alprostadil
Latanoprost

63
Q

What Drug of Prostaglandin Analogues is stated below:

▪️BN: Cytotec
▪️PGE1
▪️Effect: Cytoprotection
▪️Use: Tx. of NSAIDs- induced ulcer, abortifacient

A

Misoprostol

64
Q

What Drug of Prostaglandin Analogues is stated below:

▪️PGI2
▪️Effect: Vasodilation (systemic)
▪️Use: Mgt. of 1° Pulmonary HTN

A

Epoprestenol

65
Q

What Drug of Prostaglandin Analogues is stated below:

▪️PGE2
▪️Effect: cervical ripening
▪️Use: Therapeutic Abortion-FDA approved abortifacient

A

Dinoprostone

66
Q

What Drug of Prostaglandin Analogues is stated below:

▪️PGE1
▪️Effect: Vasodilation (local)
▪️Use: Tx. of erectile dysfunction

A

Alprostadil

67
Q

What drug is use for closure of Ductus Arteriosus

A

Indomethacin

68
Q

What Drug of Prostaglandin Analogues is stated below:

▪️BN: Xalatan
▪️PGF2a
▪️Effect: Decrease IOP
▪️Use: Antiglaucoma

A

Latanoprost (also: Carboprost)

M4: Pharmacology-Pharmacokinetics (50 decks)

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