Pharmacology GI Flashcards
what class is orlistat
lipase inhibitor
what is usage orlistat
Used as an adjunct for obese patients with a BMI ≥ 30 to lose and maintain weight
cease treatment after 12 weeks if no more than 5% change.
what receptor does orlistat work on and is it anatgonist/agonist
lipase enzyme antagonist
what is MOA orlistat
Binds to lipases, therefore preventing the breakdown and absorption of fat (triglycerides) in the duodenum.
what are side effects orlistat
Oily spotting, flatus with discharge, faecal urgency, fatty/oily stool, increased defecation and faecal incontinence
what class is methylcellulose
antihypersensitive
what is methylcellulose usage
constipation, diarrhoe, obesity
what is methylcellulose MOA
Polysacharide polymer that forms a gel in the GIT and can’t be absorbed. This gel is formed in the SI and distends it. It stimulates peristaltic activity. Also thought to suppress appetite.
what is side effects methylcellulose
mild laxative effects. flatulence
what class is atrovastatin//simvastatin
HmG-coA reductase inhibitos (statins)
what is atrovastatin/simvastain usage
Lower LDL cholesterol
Familial and non-familial
Hypercholesteremia and mixed dyslipidemia
Hypertriglyceridaemia
what receptor is atrovastin/simvastatin and is it agonist/antagonist
HmG-coA reductase, competitive antagonist
what is atrovastatin/simvastatin MOA
HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins competitively inhibit this enzyme, thereby lowering cholesterol levels.
Since cholesterol is essential for the prouction VLDL, we also see lower levels of triglycerides
what is atrovastatin/simvastatin side effects
Myalgia - common side effect of statin therapy
Diarrhoea, Joint pain, Nausea, Trouble sleeping, Stuffy nose, Sore throat
what class is cyclizine (no sedation)
anti-emetic, anti histamine
what is usage clyclizine (no sedation)
Nausea due to vertigo
Nausea due to motion sickness
Labrinythitis and menieres disease
where does cyclazine bind and its it antagonist/agonist
H1 receptor reverse agonist IT IS ANTAGONIST
what is cyclazine moa
H1 receptor has 2 states - active and inactive. The inverse agonist binds to the inactive form to reduce receptor activity
what is cyclazine side effects
drowsiness, prolong QT interval
what is promethazine(if sedation required) class
antihistamine, antipsychotic, sedative, and antiemetic
what is promethazine usage
Nausea due to vertigo
Nausea due to pregnancy
Nausea due to motion sickness. Labyrinthitis and meniere’s disease
what receptor is promaethezine and is it antagonistit/agonist
H1 receptor inverse agonist, H1 receptor anagonist
what is promoethazine moa
Bind to H1 receptors and so prevent the activation of the second messenger system stated on the left. This results in reduced hypersecretion, pruritis & sneezing
what is promethezine side effects
Drowsiness
Can’t see - blurred vision
Can’t pee - urinary retention
Can’t shit - constipation
Can’t spit - dry mouth
what class is Metoclopramide
Prochlorperazine
Domperidone
anti emetic prokinetic
what is usage of Metoclopramide
Prochlorperazine
Domperidone
Nausea due to pregnancy
Nausea due to migraine
Dysmotility dyspepsia
GORD
what receptor does Metoclopramide
Prochlorperazine
Domperidone work on and is it antagonist/agonist
D2 Gi receptor antagonist
(Dopamine Antagonist), dopamine receptor ANTAGONIST
what Metoclopramide
Prochlorperazine
Domperidone is MOA
Inhibit dopamine inhibition of ACh-induced contraction. Causes enhanced gastric emptying, reduction in the acid available to reflux and increased lower oesophageal sphincter basal tone
what is Metoclopramide
Prochlorperazine
Domperidone side effects
Parkinsonism
Tardive dyskinesia
Dystonia
Drowsiness, nervousness, agitation and anxiety
Increased pituitary prolactin release - impotence, galactorrhea, menstrual disorders
what class is metoclopramide
anti-ematic, prokinetic
what is metoclopramide usage
Nausea - migraine
Also used to treat GORD. DON’T USE REGULARLY. . Can also br used recreationally so be careful when prescribing
what is binding site of metoclopramide and is it antagonist/agonist
D2 receptor anatagonist , dopamine recepor antagonist
what is MOA of metoclopramide
Antiemetic action is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (Ach induced contraction)
Agonist effect on peripheral 5HT3 and antagonist effect on muscarinic receptors to promote gastric emptying
what is side effects of metoclopramide
Tardive dyskinesia
Parkinsonism
Hyperprolactinaemia
what class is hydocine hydrobromide (can cross BBB) so
anti ematic, anti muscaranic, anti spasmotic
what is usage of hyoscine hydrobromide (can cross bbb)
H1 receptor antagonist (antimuscarinic)
what is hyoscine hydrobromide moa
Blocks muscarinic cholinergic M1 receptors in the vestibular nuclei, the nucleus of the solitary tract and the vomitting centre. (activation of these receptors required to trigger vomitting reflex)
what is hydoscine hydrobromide side effects
Can’t see - blurred vision
Can’t pee - difficulty passing urine
Can’t spit - Dry mouth
Can’t shit - constipation
what aprepitatnt (used before chemo) is usage
only used as prevention of nausea, not whilst patient has it. Usually in cancer chemo with moderate/hight emetogenic outcomes .
what receptor binds to aprepitant (used before chemo)
NK1 antagonist - supstance P (pain) can’t bind
what is dexamthesone class
Anti-emetic
Corticosteroid
Only antiemetic given IV. Used in combo with aprepitant
what is dexamethasone usage
Post-operative nausea
Nausea due to cancer chemotherpay and radiotherapy for those at low risk pre-treatment. Don’t use in diabetic patients as can induce glucose in blood
what is dexamethasone receptor and is it agonist/antagonist
minercorticoid- 5H3 receptor antagonist
what is dexamethasone MOA
unkown
what is prochloperazaine class
anti-emetic
what is prochloperazaine usage
post-operative nausea
what is prochloperazaine binding site and is it antaginist /agonist
D2 antagonist
what is prochloperazaine MOA
inhibit stimulation of the chemoreceptor trigger zone (CTZ)
what is graniestron/ondansetron
faecal softener