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Pharm > Autocoids > Flashcards

Autocoids Flashcards

1
Q

Activation of H1 receptor

A

Vasodilation (NO induced)
Increases vascular permeability
Bronchoconstriction

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2
Q

Activation of H2 receptor

A

Increases gastric acid secretion

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3
Q

Diphenhydramine

A

1st generation H1 receptor inhibitor
Muscarinic blocker - strong
Sedation - strong
Blocks motion sickness - strong

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4
Q

Promethazine

A 
1st generation H1 receptor inhibitor
Muscarinic blocker - strong
Sedation - strong
Blocks motion sickness - moderate
Some alpha blocker and local anesthetic action
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5
Q

Chlorpheniramine

A 
1st generation H1 receptor inhibitor
Muscarinic blocker - mild
Sedation - moderate
Blocks motion sickness - moderate
May cause CNS stimulation
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6
Q

Meclizine, cyclizine, hydroxyzine

A 
1st generation H1 receptor inhibitor
Muscarinic blocker - mild
Sedation - moderate
Blocks motion sickness - strongest 
For motion sickness
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7
Q

Doxylamine

A

Includes vitamin B6

Used for morning sickness during pregnancy

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8
Q

Which are the 2nd generation H1 receptor inhibitors?

A

Cetirizine (mild sedation)
Loratadine (Claritin, most used)
Fexofenadine
No CNS entry

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9
Q

What are H1 receptor inhibitors used for?

A 
Allergic or anaphylactic reaction 
Pruritis
Allergic rhinitis, conjunctivitis
Motion sickness (imbalance signal of motion from ear and eye ---histaminergic neurons in hypothalamus----H1 and M receptor in vomiting center in medulla----nausea, vomiting)
Vertigo - meclizine
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10
Q

Side effects of H1 receptor inhibitors (1st generation)

A

Enter CNS, causing sedation; anti-muscarinic effect causing dry mouth and urine retention

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11
Q

What is the marker of carcinoid syndrome?

A

5HIAA > 25mg

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12
Q

Symptoms of carcinoid syndrome

A 
Flushing ( caused by kallikrein, the precursor of bradykinin)
Intermittent abdominal pain
Diarrhea
BP decrease
Palpitation
Wheezing
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13
Q

5-HT1 receptor

A

Gi –> decreases cAMP

Causes arterial contraction in carotid and cranial circulation

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14
Q

5-HT2 receptor

A

Gq –> increases IP3
Causes vasoconstriction, platelet aggregation, increases GI peristalsis, increases gastric acid secretion, increases vascular permeability
In the CNS it causes excitation and hallucination

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15
Q

5-HT3 receptor

A

Couples to Na+/K+ channel in the nervous system of the GIT and vomiting centre of the medulla
Causes vomiting

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16
Q

5-HT4 receptor

A

Gs –> increases cAMP

In enteric nervous system, it increases Act release –> GI motility increases

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17
Q

Sumatriptan

A

5-HT1D agonist

Used for acute migraine attacks

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18
Q

Buspirone

A

Partial 5-HT1A agonist

Used for manage anxiety

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19
Q

Clozapine, olanzapine, risperdone

A

Atypical anti-schizophrenic agents

5-HT2A antagonists

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20
Q

Cyproheptadine

A

5-HT2 and H1 antagonist

Used in carcinoid syndrome, seratonin syndrome and allergy

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21
Q

Ondansetron (and granisetron, dolasetron and alosetron)

A

5-HT3 antagonist
Central antiemetic
Used to control vomiting associated with chemotherapy
Alosetron used in IBS

22
Q

Octreotide

A

Somatostatin analog
Suppresses GI 5-HT secretion
Reduces GI motility
Supresses gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive intestinal peptide secretion
Reduces secretion of fluids by the intestine and pancreas
Vasoconstriction
Decreases portal vessel pressure, treats variceal hemorrhage

23
Q

Ergots (in general)

A

Partial agonist to alpha and 5-HT2 receptor

24
Q

LSD

A

Ergots
Lysergic acid diethylamide
5-HT2A partial agonist in CNS
Causes hallucination

25
Q

Bromocriptine, cabergoline, pergolide

A

Ergots
Agonists to dopamine D2 receptor
Used for hyperprolactinemia
Pergolide can cause valvular heart disease
Bromocriptine used for Parkinson’s disease

26
Q

Ergonovine

A

Ergots
Contract uterus
Used for obstetric bleeding, post part hemorrhage

27
Q

Ergotamine

A 
Ergots
Vasocontrictor
Contract uterus 
Used for obstetric bleeding, post part hemorrhage
Can also be used for migraine attacks
28
Q

Methysergide

A

Ergots
Vasoconstrictor
Used for diarrhea but can cause retroperitoneal fibrosis, subendocardial fibrosis, valvular disease

29
Q

Side effects of ergots

A

GI distress –> nausea, vomiting, diarrhea

30
Q

When are ergots contraindicated?

A

Coronary ischemic disease

Pregnancy

31
Q

Drugs for acute migraines

A

Ergotamine

Sumatriptan

32
Q

Drugs for prophylaxis of migraines

A

B blocker: Propranolol
Calcium channel blocker: Verapamil
Anti-histamine: Cyproheptadine
Ergot: ergonovine, methysergide

33
Q

Uses of NO

A

Pulmonary artery hypertension and acute respiratory distress syndrome in neonates - Given by inhalation
Dietary supplements with arginine: slows process of atherosclerosis

34
Q

Sildenafil MOA

A

Increases cGMP by inhibiting its breakdown by phosphodiesterase isoform 5 (PDE5)
Potentiates the actions of NO –> vasodilation

35
Q

What can happen if sildenafil is taken with nitrates?

A

Can result in severe hypotension an MI

Patients who are maintained with nitrate for ischemic heart disease should never have viagra!!!

Patients who are not on nitrate can have viagra but within 24 h should not use nitrate!!!

36
Q

Side effects of sildenafil

A

Can affect colour vision, causing difficulty in blue-green discrimination

37
Q

Which are the PDE-5 inhibitors?

A

Sildenafil, tadalafil, vardenafil

38
Q

High dose PGE2 causes:

A

Uterus relaxation

39
Q

Low dose PGE2 causes:

A

Uterus contraction

40
Q

PGE/PGI2

A

Dilation

41
Q

TXA2/PGF2a

A

Constriction

42
Q

Alprostadil

A

PGE1
Maintains a patent ductus arteriosus
Penile injection treats impotence (side effect: priapism)
Treats pulmonary hypertension (half life is 5-10min)

43
Q

Misoprostol

A

PGE1
Protects patients from NSAID-induced peptic ulcers
COX-1 enzyme expressed in stomach synthesizes PGE1 stomach mucus secretion
Mucus has cytoprotective action (protects mucosa from damage by gastric acid
Chronic use of NSAIDs or corticosteroids (CS) COX-1 activity local PGE  mucosal damage by acid leads to peptic ulcer
Can also be used with mifepristone to induce abortions

44
Q

Dinoprostone

A

PGE2

Induces labor and abortion (“cervical ripening”)

45
Q

Epoprostenol

A

PGI2
Treats pulmonary hypertension
Half life is 3-5 mins

46
Q

Latanoprost

A

PGF2a
Treats glaucoma
Side effect: dark pigment in iris

47
Q

Which drug is used to close a PDA

A

Indomethacin

48
Q

Carbaprost

A

PGF2a
Contraction of uterine muscle
Abortifacient
Postpartum bleeding

49
Q

Bosnian, ambrisentan, macitentan

A

Endothelin receptor antagonists
Treat idiopathic pulmonary arterial hypertension
ADR: flushing, headache, hypotension
Contraindication: pregnancy

50
Q

Drugs that treat idiopathic pulmonary arterial hypertension

A

Endothelin receptor antagonist (Bosentan, Ambrisentan, Macitentan)
Prostacyclin (PGI2): Epoprostenol, Iloprost, Treprostinil PDE5 inhibitor-increases cGMP: Sildenafil, Tadalafil
PGE1: Alprostadil
Nitric oxide inhalation
Guanylyl cyclase stimulator: Riociguat

Pharm (7 decks)

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