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Pharmacology > Autacoid Drugs > Flashcards

Autacoid Drugs Flashcards

1
Q

Histamine H1 receptor antagonists (group) - MoA

A

Contain an alkylamine group that resembles the side chain of histamine and permits them to bind to the H1 receptor and act as competitive receptor antagonists, and block most of the effects of histamine on vascular smooth muscles and nerves and thereby prevent or counteract allergic reactions

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2
Q

Histamine H1 receptor antagonists (group) - Clinical use

A

Allergic reactions (all are equally active for this), but differ markedly in their sedative, antiemetic and anticholinergic properties.

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3
Q

Histamine H1 receptor antagonists (group) - Interactions

A

Extensively metabolized by cytochrome P450.

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4
Q

1st generation antihistamines

A 
Chlorpheniramine
Clemastine
Dimenhydrinate
Diphenhydramine
Hydroxyzine
Meclizine
Promethazine
Doxepin
Doxylamine with vitamin B6
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5
Q

1st generation antihistamines - MoA

A

Block cholinergic muscarinic receptors

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6
Q

1st generation antihistamines - Clinical use

A

Used to produce sedation
Treat: Nausea, vomiting, vertigo.
Prevention of motion sickness.

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7
Q

1st generation antihistamines - Administration and Contraindication (Caution)

A

Administered oral or parenteral

Caution for treatment of children

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8
Q

1st generation antihistamines - Adverse effects

A 
Sedation
Children and infants: cause excitement
Dry mouth
Blurred vision
Tachycardia
Urinary retention
Hallucinations
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9
Q

Chlorpheniramine - Clinical use

A

Allergic reactions to pollen, mold, and other environmental allergens

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10
Q

Dimenhydrinate, Meclizine - Clinical use

A

Vertigo

Prevent motion sickness

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11
Q

Diphenhydramine, Hydroxyzine, Promethazine - Clinical use

A

Induce sleep, pre-op sedation.

Distress from severe pruritus

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12
Q

Doxepin - Clinical use

A

Antidepressant and anxiolytic effects
Insomnia treatment (low doses)
Induce sleep, preoperative sedation
Distress from severe pruritus

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13
Q

Doxylamine - Clinical use

A

With vitamin B6 for morning sickness in pregnant women

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14
Q

Which 1st generation antihistamines must be cautiously used against heavy machinery in patients taking the drug

A

Diphenhydramine
Hydroxyzine
Promethazine
Doxepin

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15
Q

2nd generation antihistamines + administration

A 
Cetirizine
Fexofenadine
Loratadine 
Desloratadine 
Astemizole (Removed from market)
Terfenadine (Removed from market)

Oral or parenteral

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16
Q

2nd generation antihistamines - Clinical use

A

Cause little or no sedation and are preferred for the treatment of allergic reactions
Lack antiemetic activity

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17
Q

Does 2nd generation antihistamines cross BBB?

A

No

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18
Q

Which 2nd generation antihistamine can cause some sedation?

A

Cetrizine

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19
Q

Intranasal antihistamine

A

Azelastine

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20
Q

Azelastine - Clinical use

A

Allergic rhinitis

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21
Q

Azelastine - Interaction and Contraindication (Caution)

A

Metabolized by cytochrome P450 enzymes to active metabolite, desmethylazelastine.

Caution against heavy machinery in patients taking the drug

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22
Q

Azelastine - Adverse effects

A 
Rare: 
Dizziness
Drowsiness
Headache
Fatigue
Nasal irritation
Dry mouth
Weight gain
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23
Q

Ophthalmic antihistamines

A

Levocabastine
Epinastine
Olopatadine
Ketotifen

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24
Q

Ophthalmic antihistamines - Clinical use

A

Temporary relief of symptoms of conjunctivitis

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25
Q

Levocabastine, Epinastine, Olopatadine - MoA

A

Selective H1 antagonist

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26
Q

Ketotifen - MoA

A

Selective, noncompetitive H1 antagonist and mast cell stabilizer

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27
Q

Levocabastine, Epinastine, Olopatadine - Clinical use

A

Seasonal allergic conjunctivitis

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28
Q

Ketotifen - Clinical use

A

Prevention of itching of the eye in allergic conjunctivitis

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29
Q

Ophthalmic antihistamines - Adverse effects

A

Transient stinging & burning of eyes

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30
Q

Serotonin agonists

A 
Buspirone
Sumatriptan
Triptans 
Ergot drugs 
Cisapride (Removed from market)
Tegaserod (Removed from market)
Lorcaserin
Flibanserin
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31
Q

Which serotonin agonist is a partial agonist?

A

Buspirone

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32
Q

Buspirone - MoA

A

Acts at 5-HT1A receptor

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33
Q

Buspirone - Clinical use

A

Anxiety

Depression

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34
Q

Sumatriptan (Triptans), Ergot drugs - MoA

A

Acts at 5-HT1D/1B receptor

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35
Q

Sumatriptan (Triptans), Ergot drugs - Clinical use

A

Migraine headaches

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36
Q

Lorcaserin - MoA

A

Act at 5-HT2C receptor (activates these receptors on POMC neurons located in the hypothalamus and leads to decreased food intake and promote fullness)

37
Q

Lorcaserin - Clinical use

A

Obesity

38
Q

Flibanserin - MoA

A

Acts at 5-HT1A receptor agonist and Acts at 5-HT2A receptor antagonist

39
Q

Flibanserin - Clinical use

A

Premenopausal women with hypoactive sexual desire disorder.

40
Q

Flibanserin - Adverse effects

A

Severe syncope when taken with alcohol, in individuals with hepatic dysfunction, and with certain other drugs that inhibit Flibanserin metabolism

41
Q

When can Tagaserod be used?

A

EMERGENCIES

42
Q

Serotonin antagonists

A

Clozapine, Cyproheptadine, Methysergide,

Setrons (Ondansetron, Ganisetron, Alosetron, Palonosetron, Dolasetron)

43
Q

Clozapine - MoA

A

Partially blockade of 5-HT2 receptors in CNS

44
Q

Clozapine - Clinical use

A

Schizophrenia

45
Q

Cyproheptadine - MoA

A

5-HT2 receptor antagonist with H1 antihistamine activity

46
Q

Cyproheptadine - Clinical use

A

Urticaria,
allergic reactions with pruritus,
Carcinoid tumor (with opioid antidiarrheal)

47
Q

Cyproheptadine- Adverse

A

Slight to moderate drowsiness

48
Q

Methysergide- MoA

A

5-HT2 receptor antagonist

49
Q

Methysergide - Clinical use

A

Prevent migraine headaches

50
Q

Setrons - MoA

A

Selective 5-HT3 receptor antagonist.

Prevents vomiting & nausea by blocking serotonin in chemoreceptor trigger zone and vagal afferent nerves in GI

51
Q

Setrons - Clincal use

A

Ondansetron and Ganisetron: Antiemetic (chemo and radiation therapy),
Alosetron: Women with IBS with diarrhea
Palonosetron: Prevention of acute or delayed nausea and vomiting after emetogenic cancer chemotherapy
Dolasetron: Pre-op emesis

52
Q

Serotonin reuptake inhibitors - Clinical use

A

Depression & CNS disorders

53
Q

Eicosanoid synthesis inhibitors

A

Leukotriene inhibitors, NSAIDs, Corticosteroids

54
Q

Leukotriene inhibitors - MoA

A

Inhibition of 5-lipoxygenase OR blocking leukotriene receptors

55
Q

NSAID - MoA

A

Inhibition of cyclooxygenase & prostaglandin synthesis

56
Q

Corticosteroids - MoA

A

Block formation of all eicosanoids by inhibition of phospholipase A2

57
Q

Leukotriene inhibitors - Clinical use

A

Asthma

58
Q

NSAIDs - Clinical use

A

Pain and inflammation

59
Q

Corticosteroids - Clinical use

A

Antiinflammatory, Antiallergic, Antineoplastic,

Adrenal and nonadrenal disorders

60
Q

Prostaglandin E1 + derivatives

A

Alprostadil

Misoprostol

61
Q

Misoprostol - MoA

A

Local effect on GI mucosa, cytoprotective: inh of gastric acid secretion, increases bicarbonate secretion

62
Q

Alprostadil - Clinical use

A

Maintain patent ductus arteriosis

Erectile dysfunction when other drugs are contraindicated.

63
Q

Alprostadil - Adverse effects

A

Erectile dysfunction: penile pain, fibrosis, priapism (persistent erection), flushing, diarrhea, headache, fever

64
Q

Misoprostol - Clinical use

A

Prevention of NSAID-induced gastric and duodenal ulcers

Abortifacient: combo with mifepristone (progesterone antagonist)

65
Q

Misoprostol - contraindication

A

Pregnancy

66
Q

Misoprostol - Adverse effects

A

Diarrhea (minimized with gradual increase of the dose).

Uterine contractions and premature labor

67
Q

Prostaglandin E2 and F2 alpha + derivatives

A

Dinoprostone
Carboprost
Latanoprost
Bimatoprost, travoprost and tafluprost

68
Q

Dinoprostone and Carboprost - MoA

A

Oxytocic activity and increased uterine contractions in pregnancy

69
Q

Latanoprost - MoA

A

Acts on FP receptors to increase aqueous humor outflow via the uveoscleral pathway

70
Q

Bimatoprost and travorpost - MoA

A

FP receptor agonists

71
Q

Dinoprostone - Clinical use

A

Cervical ripening before labor induction (vaginal instert, gel), Evacuate uterine contents (supp)

72
Q

Carboprost - Clincal use:

A 
Postpartum bleeding (that is resistant to other drugs)
Abortifacient
73
Q

Carboprost - Adverse effect

A

Flushing, diarrhea, vomiting, altered blood pressure, blurred vision, resp distress.

74
Q

Latonoprost - Clincal use

A

Open angle glaucoma (that is resistant to other drugs)

75
Q

Latonoprost - Adverse effect

A

Permanent eye color change (increases melanin)

76
Q

Bimatoprost and travoprost - Clinical use

A

Open angle glaucoma, ocular hypertension

77
Q

Prostaglandin I2 + derivatives

A

Epoporstenol

Treprostinil

78
Q

Epoprostenol – MoA

A

Acts on IP receptors to dilate pulmonary blood vessels and increase pulmonary blood flow

79
Q

Epoprostenol and Treprostinil - Clinical use

A

Pulmonary arterial hypertension (reduce symptoms associated with exercise)

80
Q

Epoprostenol - Adverse effects

A

Flushing, tachycardia, hypotension, diarrhea, nausea, vomiting, flulike symptoms

81
Q

Endothelin-1 antagonists

A

Bosentan
Ambrisentan
Macitentan

82
Q

Endothelin-1 antagonists - Clinical use

A

Pulmonary arterial hypertension

83
Q

Bosentan - Contraindication

A

Pregnancy, women in childbearing age not on hormonal contraceptives

84
Q

Bosentan - Adverse effects

A 
Elevated aminotransferase levels. 
Birth defects (animal studies)
85
Q

Sildenafil - Classification

A

PDE5 inhibitor

86
Q

Sildenafil - MoA

A

Increases cyclic guanosine monophosphate within pulmonary vascular smooth muscle cells, results in relaxation and vasodilation of the pulmonary vascular bed

87
Q

Sildenafil - Clinical use

A

Pulmonary arterial hypertension

Sexual dysfunction

88
Q

Clemastine - Clinical use

A

Allergic rhinitis, Hay fever, pruritus

Pharmacology (55 decks)

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