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Pharmacology > Autocoids > Flashcards

Autocoids Flashcards

1
Q

Autocoids include

A

Amines
Vasaactive peptides
Fatty acids derivatives

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2
Q

Histamine

A

Calcium dependent- penicillin
Calcium independent - vancomycin and morphine

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3
Q

Receptors

A

H1- Gq and vasodilation (so increasing permeability and causing oedema)
H2 - Gs (also has some VD on it’s own BV’s but like…)
*Above G coupled protein receptors
H3 - nerve endings nd CNS
H4 - inflammatory response

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4
Q

Itching, urticaria and pain

A

H1

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5
Q

GIT and heart

A

H2

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6
Q

Histamine Antagonists
Physiological antagonists- adrenaline through:

A

H1 receptor (anti h) - allergy
H2 receptors to decrease gastric secretion - cimetidine, ranitidine

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7
Q

First generation anti histaminics- pass bbb so sedation
Block autonomic receptors (muscarinic so has atropine like action) and 4 to 6 hrs only

A

Dimenhydrinate
*Diphenhydramine
Clemastine
Chlorpheniramine
Cyclizine
Meclizine
Carbinoxamine
Cyproheptadine - in unoperable carcinoid syndrome producing excess serotonin
*Promethazine
Hydroxyzine
*in preventing vomiting in motion sickness because H1 and muscarinic blocking

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8
Q

Second generation
No bbb
No blockage
12 to 24 hrs

A

Fexofenadine
Loratidine
Cetirizine

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9
Q

2nd generation adverse effects

A

Cyt p450
Prolonged QT interval and serious arrhythmia (torsade de pointes) with drugs that inhibit cyp450 - ketoconazole and erythromycin

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10
Q

Potentiate sedative effectbof hypnotics

A

1st generation

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11
Q

Taken with drugs that inhibit their metabolism (CYP450 inhibitors)

A

2nd generation

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12
Q

Serotonin has

A

7 receptors

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13
Q

Serotonin 2

A

VC except skeletal bv
Platelet aggregation
Contraction of smooth muscles for peristalsis

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14
Q

S3

A

Reflex bradycardia and hypotension carried by vagus

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15
Q

S4

A

Acetylcholine release fuf o⁷⁷

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16
Q

Serotonin affects

A

CVS
GIT
Nervous System

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17
Q

Sero Agonists

A

Buspirone - non diazepene antianxiety that takes 2 weeks to appear.

Sumatritan and zolmitritan (short duration multiple but doses 2 per day- coronary vasospasm so contraindicated in angina, hypertension and the rest

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18
Q

S1

A

A - anti Anxiety
B/D - VC

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19
Q

Dexfenfluramine

A

Appetite suppression but cardiac valve defect

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20
Q

Ito and cisapride

A

Prokinetics for GERefluxDisease

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21
Q

Tegaserod - selective s4

A

Motility- in IBS and predominant constipation

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22
Q

Escitalopram, Fluoxetine and fluvolamine

A

Serotonin reuptake inhibitors
For depression and others

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23
Q

Agonists

A

Buspirone
Sulma and zomitriptan
Dexfenfluramine
Ito and cisapride
Tegaserod
Escitalopram, Fluoxetine and fluvolamine

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24
Q

Antagonists

A

Cyproheptadine - for prophylaxis of migraine through S2 blockade (VD)
Ketanserin - carcinoid syndrome (blocks S2) for bronchospasm and hypertension
Odan and granisetron - block S3

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25
Q

Ergot alkaloids- SUDA

A

Serotonin
Uterus
Dopamine
Alpha adrenergic receptors

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26
Q

Ergot alkaloids

A

Migraine
-ergotamine tartrate (all routes) for prodrome of the attack and usually combined with caffeine to facilitate it’s absorption
Hyperprolactinemia
-Bromocriptine - reducing prolactin, suppress physiologic lactation and regression of the tumours(small maybe)
-Cabergoline - stronger
Postpartum hemorrhage
-Ergometrine (tamine can cause abortion)

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27
Q

Amputation in

A

Vasospasm by ergots
Treat with infusion of large doses of ONLY nitroprusside or nitroglycerin

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28
Q

Vaso active peptide

A

Constrictors - angiotensin 2, vasopressin, neuropeptide Y, endothelin
Dilators - bradykinin, natiuretic peptides, substance P, VIP, neurotensin

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29
Q

ACE

A

Kininase 2
Dipeptidyl carboxy peptidase

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30
Q

Renin receptor blockers

A

EnalkiREN
RemikiREN

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31
Q

Metabolises other substances like bradykinin and substance P

A

ACE

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32
Q

ACE inhibitors

A

CaptoPRIL
LisinoPRIL
EnalaPRIL

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33
Q

40 times nor adr and increases its release

A

Angiotensin 2 - VC
Stimulates sympathetic ganglia and adrenal medulla

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34
Q

Angiotensin

A

Increase nor adrenaline, aldosterone angiotensinogen ADH and ACTH(dipsogenic effect - increased ddrinking)
Decreases renin negative feedback
Has mitogenic - hypertrophy remodelling of the heart and bv
Spasmogenic effect on bvs

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35
Q

RAAS inhibitors

A

Beta blockers- decrease renin
Renin receptor blockers on angiotensinogen
ACE inhibitors
Angiotensin type 1 receptor blockers - losartan, valsartan, candersartan and telmisartan

36
Q

Kinin from

A

Kininogen through kallikrein

37
Q

Kinins rapidly metabolised by

A

Kininase so t1/2 15 secs

38
Q

HMWK

A

Bradykinin in plasma
B2 > B1

39
Q

LMWK

A

Lys - bradykinin (kallidin) in tissue
B2 = B1

40
Q

10 times VD effect of histamine

A

Kinin
-stimulate B2 and increase Prostaglandin

41
Q

Venous VC (increase venous pressure) but arteriolar VD

42
Q

Oedema, pain

A

Increased capillary permeability and stimulation of sensory nerve endings by kinins
Kinin us spasmogenic despite VD

43
Q

Icatibant (sc)
Selective B2 receptor antagonists

A

2nd generation decapeptide for acute attacks of hereditary angioedema

44
Q

Inhibits kallikrein enzymes for synthesis of kinin

45
Q

ETa receptors
Too much in case of pulmonary hypertension, HF and CAD

A

VC vascular smooth muscles proliferation, cardiac hypertrophy and elevation of bp

46
Q

Bosentan (orally)

A

Non selective for both ETa and ETb

47
Q

Ambrisentan

A

Selective ETa

48
Q

Arachidonic acid

A

COX - PG
LOX - leukotrienes, lipoxins

49
Q

Protective PG(E2 and I2)

A

COX 1
Protects stomach from HCL and renal blood flow regulation

50
Q

In inflammatory cells

A

COX2 for increasing prostanoids

51
Q

Variant of COX 2 (COX Ib) in the brain only

A

COX 3 central
PG for pain and fever
Inhibited by paracetamol

52
Q

Prostanoid receptors

A

DP D2
FP 2alpha
IP I2
EP E2 - EP1 EP2 EP3 EP5
TP TXA2

53
Q

TXA2 PGI2 balance on CVS

A

Platelet function and vascular tone control

54
Q

E and D

55
Q

F2alpha and TXA2

56
Q

E2 and I2

A

Cytoprotective effect on GIT
-Reduced HCL
- Increased mucus
-VD
And autoregulatory renal function rogether with E1

57
Q

E2

A

Pyrexia with EP 3 on CNS via IL1 stimulation

58
Q

All of PGE and PGF

A

Lower IOP increase outflow from anterior chamber uveoscleral

59
Q

E2 and F2alpha for female

A

Potent oxytocic action(uterine contractions)
-Dinoprostone

60
Q

PGE1
*Misoprostol (oral) -NSAID peptic ulcer

A

Penile erection
-Alprosradil (IV)as urethral jnsert on corpus cavernosum

61
Q

PG in male

A

Seminal V. Prostate and testis
*Alprostadil - treatment of erectile dysfunction in men as urethral insert
-VD of corpus spongiosum

62
Q

Epoprostenol IV

A

PGI2 gif pulmonary hypertension

63
Q

Latanoprast

A

Open angle glaucoma eye drop

64
Q

B4 C4 D4 E4

A

Slow reacting substance of Anaphylaxis - C D and E
B is just a leukotriene

65
Q

Inhibitors of eicosanoids

A

Glucocorticoids inhibit all(phospholipase A2
NSAIDS (aspirin nonselective and celecoxib selective) - anti inflammatory analgesic and pyretic
Dazoxiben - inhibits TAX2
Anti leukotriene - zafirlukastand montelukast
Zileuton inhibits 5 lipooxygenase to decrease LTs

66
Q

Migraine

A

Vascular and neuronal recurrent episodic pain

67
Q

Pathop1 of migraine through

A

VD secondary to intracranial VC and cerebral hypoxia

68
Q

Pathop2 of migraine through

A

Activation of trigeminal nerve
Release of
-CANVAS
-Calcitonim gene related peptide (CGRP)
-Neuropeptide Y
- VIP
-Substance P
Vasodilation of bev of cranium and dura matter and extravasation of pp
Mast cell degran and nociceptor activation

69
Q

Phases

A

Prodrome - vague 24hrs
Aura - focal neurologic hr
Migraine itself
Resolution with sleep

70
Q

Acute non specific

A

NSAIDS and Antiemetics

71
Q

Acute specific

A

Triptans
Dihdroergotamine

72
Q

Ergot alkaloids - serotonin and alpha agonist for VC plus Dopamine causing emesis
*dihydro - no emesis

A

Amino acid - tamine and toxine
Amine - metrine
Semisynthetic derivatives- Methyl ergoMetrine, dihydro ergotamine and toxine

73
Q

Increase ergot absrption plus mood

74
Q

Ergots touch
All routes administration

A

Chemoreceptor Trigger Zone causing nausea and vomiting plus CIC plus bradycardia

75
Q

Di hydro ergotamine has

A

More alpha and less emesis than ergotamine

76
Q

Triptans suma and zomi

A

Short duration but 2 doses per day and 4 days per month

77
Q

Fewer coronary sapsm side effects

A

Naratriptan

78
Q

Mild attacks of migraine

A

Analgesic like paracetamol (NSAID) but not in pregnancy plus ibuprofen and naproxen
And antiemetics like metoclopramide and domperidone

79
Q

Severe attacks

A

Ergots (tamine and dihydro) or Triptans +- antiemetic

80
Q

Prophylaxis in migraine

A

Asymptomatic between attacks

81
Q

Prophylactic drugs

A

Beta blocker - propranolol and timolol stabilise brain and excitability and anxiety
Plus stabilise serotonin (so no VC)
Antidepressant TCA and NOT SSRI(selective serotonin uptake inhibitor like fluoxetine, fluvoxamine and escitalopram)- VD and Na channel blocking

82
Q

More prophylactic drugs

A

Anticonvulsant like topiramate and sodium valproate -targets pathop2 for trigeminal
CCB like verapamil - VD decreased excitability and neurotransmitter release
Aimovig (Erenumab) sc- blocks CGRP release

83
Q

No SSRI in depression migraine

A

As it increases serotonin- VC and serotonin syndrome

84
Q

Use of antihistaminics is inieffectives in bronchial asthma

A

As bronchial asthma usually invoices many mediators

85
Q

Most potent antiemetics

A

Diphenhydramine and promethazine

Pharmacology (17 decks)

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