Term
What are the histamine receptors & where are they located on our body?
Function? |
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Definition
H1 - blood vessel -
Vasodilation
Bronchoconstriction
= anaphylaxis
H2 - stomach
Increase in gastric secreations |
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Term
Name the 1st generation H1 antihistamines
AKA? |
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Definition
Sedating antihistamines
Diphenhydramine
Chlorpheniramine
Promethazine
Hydroxyzine |
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Term
Name the 2nd generation H1 antihistamines
AKA? |
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Definition
NONSEDATING
Loratidine (claritin)
Fexofenadine (allegra)
Cetirizine (zyrtec)
Azelastin (intranasal spray) |
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Term
| Which antihistamines are used to treat the EPS of Parkinson's disease? |
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Definition
Diphenhydramine
Promethazine (anticholinergics) |
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Term
| What are the actions of antihistamines? |
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Definition
•Antiallergic
Antagonise histamine induced bronchoconstriction, urticaria
•CNS
Sedation - 1st generation drugs
Prevent motion sickness
Cough suppressant-chlorpheniramine
•Anticholinergic- Promethazine, diphenhydramine
reduce tremor, rigidity- Parkinsonism
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Term
| What are the ADR's associated with antihistamines? |
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Definition
Similar to anticholinergics
urinary hesitancy, blurring of vision, dry mouth |
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Term
Name the H2 antagonists
Use? |
|
Definition
Cimetidine,
Ranitidine,
Famotidine
Clinical use- Acid-peptic disease (Duodenal/gastric ulcer)
Zollinger-Ellison syndrome- characterized by acid hypersecretion, severe peptic ulceration, GI bleeding
Gastroesophageal reflux disease
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Term
| What are the serotonin receptors & where are they found? |
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Definition
5-HT1 & 5-HT2 receptors- present both in CNS & peripheral tissue
5 HT3 –receptors- found in chemoreceptor trigger zone(area posterema) & vomiting centre in CNS
peripheral & enteric nerves
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Term
Name the 5-HT1 receptor agonists
Use? |
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Definition
Sumatriptan - 5 HT1D agonist - acute migraine attack
Buspirone - anxiolytic drug (treats anxiety) – 5HT1a agonist
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Term
| Name the 5HT4 - Receptor Agonists |
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Definition
Tegaserod - used in irritable bowel syndrome when associated with constipation - 5HT4 agonist
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Term
5 HT2 receptor antagonists
ADR's |
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Definition
Ketanserine
Olanzapine
Cyproheptadine
ADR: diarrhoea, flushing (vasodilatation) & bronchoconstriction
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Term
|
Definition
| 5 HT2 & alpha adrenoceptor blocker |
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Term
|
Definition
5HT2 antagonist
- used in carcinoid tumours - tumour that secretes serotonin
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Term
| Name the 5HT3 receptor antagonists |
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Definition
|
Ondansetron,
Granisetron,
Dolasetron,
Alosetron
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Term
| Use of the 5HT3 receptor antagonists |
|
Definition
Central antiemetic action
Clinical Uses:
–control of vomiting associated with chemotherapy
–Alosetron used in irritable bowel syndrome
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Term
| What are the Ergots that are used in postpartum haemorrhage & why? |
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Definition
|
–Ergonovine & Ergotamine - acts on the uterus - stops bleeding
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Term
| What ergots are used in hyperprolactinemia? |
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Definition
|
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Term
| What Ergot is used to treat carcinoid tumour? |
|
Definition
Methysergide
(also somatostatin analogue Octreotide)
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Term
| What is the Nitric oxide synthases (NOS) Donor? |
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Definition
|
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Term
| What are the actions of NO? |
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Definition
| Powerful vasodilator - SMOOTH MUSCLE relaxant - via increase in cGMP |
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Term
| What are the approved uses of NO |
|
Definition
Pulmonary artery hypertension,
Acute respiratory distress syndrome in neonates - Given by inhalation
Dietary supplements with arginine: slows process of atherosclerosis
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Term
What is drug used in erectile dysfunction?
MOA?
Drug reactions? |
|
Definition
Sildenafil (viagra)
Increases cGMP by inhibiting its breakdown by phosphodiesterase isoform 5
If used with NO (for angina) MI can occur, as it potentiates the actions of NO. |
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Term
|
Definition
Prostaglandins
Thromboxanes
Leukotrienes |
|
|
Term
In some cyanotic heart diseases such as TGV - Transposition of the great vessels - the Ductus Arteriosus must be kept open
what drug is used to achieve this?
What is another use of this drug? |
|
Definition
PGE1 (prostoglandin) - alprostadil
vasodilator - induces penile erection in dysfunctional male
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Term
| What is used to treat NSAID induced peptic ulcer? |
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Definition
|
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Term
|
Definition
Used with mifepristone(antiprogestin) - to induce abortions
Treats NSAID induced peptic ulcer
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Term
What prostaglandins are used in cervical ripening & abortificants?
How? |
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Definition
|
Dinoprostone (PGE2)
Carboprost (PGF 2α)
Causes contraction of uterine muscles |
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Term
What causes Dysmenorrhea?
How can it be treated?
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Definition
Increases endometrial synthesis of PGE2 and PGF2a during menstruation
NSAIDs (ibuprofen) inhibit the synthesis of these PGs thus relieve pain
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Term
|
Definition
Synthetic PGE1 - Vasodilator
- TGV - Transposition of great valves
-Induces erection in dysfunctional males |
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Term
What prostaglandin is used in pulmonary hypertension?
Why? |
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Definition
PGI2 (epoprostenol) - it is a platelet stabilizer and vasodilator
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|
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Term
| What prostaglandin is used in Glaucoma & how? |
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Definition
| Latanoprost - increase in AQH outflow |
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Term
Leukotrienes
How are they formed?
Types & uses? |
|
Definition
Arachidonic acid.. via
Lipoxygenase.. forms
Hydroperoxidase.. then forms
Leukotrienes
LTB4 - inflammatory mediator - neutrophil chemoattractant
LTA4, LTC4, LTD4 - cause anaphylaxis |
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Term
How can the formation of leukotrienes be inhibited?
Use? |
|
Definition
Lipoxygenase enzyme inhibitors - Zileuton
LT receptor antagonists - Zafirllukast, Monteleukast
Phospholipase A2 inhibitors - Corticosteroids
Use: Bronchial asthma |
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Term
| How are prostaglandin's & Thromboxanes formed? |
|
Definition
Arachidonic acid via
Cox 1 & 2 .. forms
Endoperoxides.. which form
PG's |
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