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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
Levocabastine, Epinastine, Olopatadine - MoA
Selective H1 antagonist
26
Ketotifen - MoA
Selective, noncompetitive H1 antagonist and mast cell stabilizer
27
Levocabastine, Epinastine, Olopatadine - Clinical use
Seasonal allergic conjunctivitis
28
Ketotifen - Clinical use
Prevention of itching of the eye in allergic conjunctivitis
29
Ophthalmic antihistamines - Adverse effects
Transient stinging & burning of eyes
30
Serotonin agonists
``` Buspirone Sumatriptan Triptans Ergot drugs Cisapride (Removed from market) Tegaserod (Removed from market) Lorcaserin Flibanserin ```
31
Which serotonin agonist is a partial agonist?
Buspirone
32
Buspirone - MoA
Acts at 5-HT1A receptor
33
Buspirone - Clinical use
Anxiety | Depression
34
Sumatriptan (Triptans), Ergot drugs - MoA
Acts at 5-HT1D/1B receptor
35
Sumatriptan (Triptans), Ergot drugs - Clinical use
Migraine headaches
36
Lorcaserin - MoA
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
Lorcaserin - Clinical use
Obesity
38
Flibanserin - MoA
Acts at 5-HT1A receptor agonist and Acts at 5-HT2A receptor antagonist
39
Flibanserin - Clinical use
Premenopausal women with hypoactive sexual desire disorder.
40
Flibanserin - Adverse effects
Severe syncope when taken with alcohol, in individuals with hepatic dysfunction, and with certain other drugs that inhibit Flibanserin metabolism
41
When can Tagaserod be used?
EMERGENCIES
42
Serotonin antagonists
Clozapine, Cyproheptadine, Methysergide, | Setrons (Ondansetron, Ganisetron, Alosetron, Palonosetron, Dolasetron)
43
Clozapine - MoA
Partially blockade of 5-HT2 receptors in CNS
44
Clozapine - Clinical use
Schizophrenia
45
Cyproheptadine - MoA
5-HT2 receptor antagonist with H1 antihistamine activity
46
Cyproheptadine - Clinical use
Urticaria, allergic reactions with pruritus, Carcinoid tumor (with opioid antidiarrheal)
47
Cyproheptadine- Adverse
Slight to moderate drowsiness
48
Methysergide- MoA
5-HT2 receptor antagonist
49
Methysergide - Clinical use
Prevent migraine headaches
50
Setrons - MoA
Selective 5-HT3 receptor antagonist. | Prevents vomiting & nausea by blocking serotonin in chemoreceptor trigger zone and vagal afferent nerves in GI
51
Setrons - Clincal use
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
Serotonin reuptake inhibitors - Clinical use
Depression & CNS disorders
53
Eicosanoid synthesis inhibitors
Leukotriene inhibitors, NSAIDs, Corticosteroids
54
Leukotriene inhibitors - MoA
Inhibition of 5-lipoxygenase OR blocking leukotriene receptors
55
NSAID - MoA
Inhibition of cyclooxygenase & prostaglandin synthesis
56
Corticosteroids - MoA
Block formation of all eicosanoids by inhibition of phospholipase A2
57
Leukotriene inhibitors - Clinical use
Asthma
58
NSAIDs - Clinical use
Pain and inflammation
59
Corticosteroids - Clinical use
Antiinflammatory, Antiallergic, Antineoplastic, | Adrenal and nonadrenal disorders
60
Prostaglandin E1 + derivatives
Alprostadil | Misoprostol
61
Misoprostol - MoA
Local effect on GI mucosa, cytoprotective: inh of gastric acid secretion, increases bicarbonate secretion
62
Alprostadil - Clinical use
Maintain patent ductus arteriosis | Erectile dysfunction when other drugs are contraindicated.
63
Alprostadil - Adverse effects
Erectile dysfunction: penile pain, fibrosis, priapism (persistent erection), flushing, diarrhea, headache, fever
64
Misoprostol - Clinical use
Prevention of NSAID-induced gastric and duodenal ulcers | Abortifacient: combo with mifepristone (progesterone antagonist)
65
Misoprostol - contraindication
Pregnancy
66
Misoprostol - Adverse effects
Diarrhea (minimized with gradual increase of the dose). | Uterine contractions and premature labor
67
Prostaglandin E2 and F2 alpha + derivatives
Dinoprostone Carboprost Latanoprost Bimatoprost, travoprost and tafluprost
68
Dinoprostone and Carboprost - MoA
Oxytocic activity and increased uterine contractions in pregnancy
69
Latanoprost - MoA
Acts on FP receptors to increase aqueous humor outflow via the uveoscleral pathway
70
Bimatoprost and travorpost - MoA
FP receptor agonists
71
Dinoprostone - Clinical use
Cervical ripening before labor induction (vaginal instert, gel), Evacuate uterine contents (supp)
72
Carboprost - Clincal use:
``` Postpartum bleeding (that is resistant to other drugs) Abortifacient ```
73
Carboprost - Adverse effect
Flushing, diarrhea, vomiting, altered blood pressure, blurred vision, resp distress.
74
Latonoprost - Clincal use
Open angle glaucoma (that is resistant to other drugs)
75
Latonoprost - Adverse effect
Permanent eye color change (increases melanin)
76
Bimatoprost and travoprost - Clinical use
Open angle glaucoma, ocular hypertension
77
Prostaglandin I2 + derivatives
Epoporstenol | Treprostinil
78
Epoprostenol – MoA
Acts on IP receptors to dilate pulmonary blood vessels and increase pulmonary blood flow
79
Epoprostenol and Treprostinil - Clinical use
Pulmonary arterial hypertension (reduce symptoms associated with exercise)
80
Epoprostenol - Adverse effects
Flushing, tachycardia, hypotension, diarrhea, nausea, vomiting, flulike symptoms
81
Endothelin-1 antagonists
Bosentan Ambrisentan Macitentan
82
Endothelin-1 antagonists - Clinical use
Pulmonary arterial hypertension
83
Bosentan - Contraindication
Pregnancy, women in childbearing age not on hormonal contraceptives
84
Bosentan - Adverse effects
``` Elevated aminotransferase levels. Birth defects (animal studies) ```
85
Sildenafil - Classification
PDE5 inhibitor
86
Sildenafil - MoA
Increases cyclic guanosine monophosphate within pulmonary vascular smooth muscle cells, results in relaxation and vasodilation of the pulmonary vascular bed
87
Sildenafil - Clinical use
Pulmonary arterial hypertension | Sexual dysfunction
88
Clemastine - Clinical use
Allergic rhinitis, Hay fever, pruritus

Pharmacology (55 decks)

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