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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
Ergot alkaloids- SUDA
Serotonin Uterus Dopamine Alpha adrenergic receptors
26
Ergot alkaloids
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)
27
Amputation in
Vasospasm by ergots Treat with infusion of large doses of ONLY nitroprusside or nitroglycerin
28
Vaso active peptide
Constrictors - angiotensin 2, vasopressin, neuropeptide Y, endothelin Dilators - bradykinin, natiuretic peptides, substance P, VIP, neurotensin
29
ACE
Kininase 2 Dipeptidyl carboxy peptidase
30
Renin receptor blockers
EnalkiREN RemikiREN
31
Metabolises other substances like bradykinin and substance P
ACE
32
ACE inhibitors
CaptoPRIL LisinoPRIL EnalaPRIL
33
40 times nor adr and increases its release
Angiotensin 2 - VC Stimulates sympathetic ganglia and adrenal medulla
34
Angiotensin
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
35
RAAS inhibitors
Beta blockers- decrease renin Renin receptor blockers on angiotensinogen ACE inhibitors Angiotensin type 1 receptor blockers - losartan, valsartan, candersartan and telmisartan
36
Kinin from
Kininogen through kallikrein
37
Kinins rapidly metabolised by
Kininase so t1/2 15 secs
38
HMWK
Bradykinin in plasma B2 > B1
39
LMWK
Lys - bradykinin (kallidin) in tissue B2 = B1
40
10 times VD effect of histamine
Kinin -stimulate B2 and increase Prostaglandin
41
Venous VC (increase venous pressure) but arteriolar VD
Kinin
42
Oedema, pain
Increased capillary permeability and stimulation of sensory nerve endings by kinins Kinin us spasmogenic despite VD
43
Icatibant (sc) Selective B2 receptor antagonists
2nd generation decapeptide for acute attacks of hereditary angioedema
44
Inhibits kallikrein enzymes for synthesis of kinin
Aspirin
45
ETa receptors Too much in case of pulmonary hypertension, HF and CAD
VC vascular smooth muscles proliferation, cardiac hypertrophy and elevation of bp
46
Bosentan (orally)
Non selective for both ETa and ETb
47
*A*mbrisentan
Selective ET*a*
48
Arachidonic acid
COX - PG LOX - leukotrienes, lipoxins
49
Protective PG(E2 and I2)
COX 1 Protects stomach from HCL and renal blood flow regulation
50
In inflammatory cells
COX2 for increasing prostanoids
51
Variant of COX 2 (COX Ib) in the brain only
COX 3 central PG for pain and fever Inhibited by paracetamol
52
Prostanoid receptors
DP D2 FP 2alpha IP I2 EP E2 - EP1 EP2 EP3 EP5 TP TXA2
53
TXA2 PGI2 balance on CVS
Platelet function and vascular tone control
54
E and D
BromchiD
55
F2alpha and TXA2
BronchoC
56
E2 and I2
Cytoprotective effect on GIT -Reduced HCL - Increased mucus -VD And autoregulatory renal function rogether with E1
57
E2
Pyrexia with EP 3 on CNS via IL1 stimulation
58
All of PGE and PGF
Lower IOP increase outflow from anterior chamber uveoscleral
59
E2 and F2alpha for female
Potent oxytocic action(uterine contractions) -Dinoprostone
60
PGE1 *Misoprostol (oral) -NSAID peptic ulcer
Penile erection -Alprosradil (IV)as urethral jnsert on corpus cavernosum
61
PG in male
Seminal V. Prostate and testis *Alprostadil - treatment of erectile dysfunction in men as urethral insert -VD of corpus spongiosum
62
Epoprostenol IV
PGI2 gif pulmonary hypertension
63
Latanoprast
Open angle glaucoma eye drop
64
B4 C4 D4 E4
Slow reacting substance of Anaphylaxis - C D and E B is just a leukotriene
65
Inhibitors of eicosanoids
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
Migraine
Vascular and neuronal recurrent episodic pain
67
Pathop1 of migraine through
VD secondary to intracranial VC and cerebral hypoxia
68
Pathop2 of migraine through
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
Phases
Prodrome - vague 24hrs Aura - focal neurologic hr Migraine itself Resolution with sleep
70
Acute non specific
NSAIDS and Antiemetics
71
Acute specific
Triptans Dihdroergotamine
72
Ergot alkaloids - serotonin and alpha agonist for VC plus Dopamine causing emesis *dihydro - no emesis
Amino acid - tamine and toxine Amine - *m*etrine Semisynthetic derivatives- Methyl ergoMetrine, dihydro ergotamine and toxine
73
Increase ergot absrption plus mood
Cafergot
74
Ergots touch All routes administration
Chemoreceptor Trigger Zone causing nausea and vomiting plus CIC plus bradycardia
75
Di hydro ergotamine has
More alpha and less emesis than ergotamine
76
Triptans suma and zomi
Short duration but 2 doses per day and 4 days per month
77
Fewer coronary sapsm side effects
Naratriptan
78
Mild attacks of migraine
Analgesic like paracetamol (NSAID) but not in pregnancy plus ibuprofen and naproxen And antiemetics like metoclopramide and domperidone
79
Severe attacks
Ergots (tamine and dihydro) or Triptans +- antiemetic
80
Prophylaxis in migraine
Asymptomatic between attacks
81
Prophylactic drugs
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
More prophylactic drugs
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
No SSRI in depression migraine
As it increases serotonin- VC and serotonin syndrome
84
Use of antihistaminics is inieffectives in bronchial asthma
As bronchial asthma usually invoices many mediators
85
Most potent antiemetics
Diphenhydramine and promethazine
86
Ibuprofen Naproxen
Mild analgesic
87
Meyoclopramide Domperidone (parenteral or rectal(
Anti emetic

Pharmacology (27 decks)

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