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PharmacologyII > Pre-Midterm Drugs > Flashcards

Pre-Midterm Drugs Flashcards

1
Q

what is salbutamol and terbutaline used for? whats is its MOA?

A
  • asthma, bronchodilator.

- β2 agonist that is GPCR–> increases cAMP–>activate PKA and reduces calcium levels which cause bronchodilation.

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2
Q

what is the main difference between salbutamol/ terbutaline and salmeterol/ formoterol?

A

both have the same MOA and adverse effects but salmeterol and formoterol are longer lasting (8-12 hours) rather than 3-5 hours.

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3
Q

what are the side effects salbutamol, terbutaline, salmeterol and formoterol?

A
  • tachycardia, dysrhythmias, tremor (β2 agonist also have an effect on the heart which is caused by increasing the calcium levels).
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4
Q

what is theophylline/ aminophylline? what is the MOA?

A
  • asthma drugs (Methylxanthine based agents), bronchodilators.
  • main one: inhibits phosphodiesterase–> high cAMP –> bronchodilation.
    others: inhibits adenosine receptors (which cause bronchoconstriction) and inhibit the release of Intracellular calcium.
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5
Q

what are the adverse effects of methylxanthine based agents for asthma? (theophylline and aminophylline)

A
  • dysrythmia and seizures.
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6
Q

what is montelukast/zafirlukast? what is the MOA? do they have any major side effects?

A
  • asthma drugs, bronchodilators.
  • work by antagonizing Cysteinyl leukotriene receptors (specifically cysLT1- Gq). cause bronchodilation, reduces mucous, reduces hyperesponsive airways.
  • No, well tolerated.
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7
Q

what are 4 classes of drugs that are bronchodilators for asthma?

A

1- β2 agonists
2- PDE inhibitors or theophylline/ aminophylline
3- CysLt receptor antagonists
4- muscarinic receptor antagonists.

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8
Q

what are beclometasone, budenoside, fluticasone, mometasone, ciclesonide and prednisolone. what is the difference between the first 5 drugs and prednisolone?

A

these are glucocorticoids that are used for asthma. they are anti-inflammatory agents, prevents the progression of chronic asthma. the first 5 drugs are given via inhalation but prednisolone is given orally.

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9
Q

what is the MOA of beclometasone, budenoside, fluticasone, mometasone, ciclesonide and prednisolone?

A
  • general: they are glucocorticoids, bind intracellular receptors and dimerize, allows nuclear translocation and modification of gene transcription. could work by basic transactivation or basic transrepression and the transrepression is more relavent because ligand binds to GR dimer and it turns of transcription.
  • specific: reduction in IL2 gene reduces the formation of th2 cytokines= less recruitment of eosinophiles which inhibits the allergen induced influx of eosinophiles into the lungs (by decreasong IL-5/IL-13). this reduces the production of IgE and IgE receptors.
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10
Q

what is the MOA of beclometasone, budenoside, fluticasone, mometasone, ciclesonide and prednisolone?

A

they are glucocorticoids, bind intracellular receptors and dimerize, allows nuclear translocation and modification of gene transcription.

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11
Q

MOA of 5-HT3 Receptor Antagonists

A
  • inhibit vagal signaling to the emetic center in the brainstem and also slow intestinal transit
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12
Q

Adverse Effect of 5-HT3 Receptor Antagonists

A
  • generally well tolerated
  • headache and GI upset (constipation)
  • ischemic colitis (alosetron)
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13
Q

what is ipratropium/tiotropoium used for? what is the MOA.

A
  • asthma/ COPD drug. (derived from atropine)
  • parasympathetic stimulation of muscarinic receptors (m3- Gq) on the bronchioles = high calcium so contraction of smooth muscles. so we would need anti-muscarinic or anti-cholinergic drugs to cause bronchodilation.
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14
Q

what are some side effects of glucocorticoids used for asthma?

A
  • oropharyngeal candidiasis (thrush)

- adrenal suppression (in childen, issue with baclometasone and budenoside only).

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15
Q

What are the antipsychotic phenothiazines?

A
  • chlorpromazine
  • perphenazine
  • prochlorperazine
  • trifluoperazine
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16
Q

Chlorpromazine, perphenazine, prochlorperazine, and trifluoperazine are examples of what? And are used to treat?

A
  • examples of Dopamine receptor 2 (D2) antagonists

- are used for treatment of severe nausea and vomiting

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17
Q

MOA of D2 antagonists

A
  • D2 receptors are linked to Gi proteins which inhibit adenylyl cyclase, thereby reducing cAMP formaiton and activation of protein kinase A
  • D2 antagonist therefore reverse the inhibitory action of D2 receptors
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18
Q

Adverse effects of D2 antagonists

A
  • extrapyramidal syndrome
  • dystonias
  • tardive dyskinesia
  • hyperprolactinemia
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19
Q

Metoclopramide/Domperidone and adverse effects

A
  • D2 antagonists antiemetic drugs

- Adverse effects: spasmodic torticollis, occulogyric crises, stimulated prolactin release

20
Q

Difference between Metoclopramide and Domperidone

A
  • domperidone does not penetrate the blood brain barrier (BBB) so there is less CNS side effects
21
Q

Haloperidol, droperidol, and levomepromazine

A
  • other D2 receptor antagonists used against acute chemotherapy-induced emesis
22
Q

Histamine H1 Receptor Antagonists

A
  • cinnarizine
  • cyclizine
  • promethazine
23
Q

what is omalizumab and what is its MOA?

A
  • asthma drug thats used to treat severe allergic asthma that doesnt respond to high doses of corticosteroids.
  • MOA: monoclonal anti- IgE antibody, binds to IgE and prevents their interaction with other receptors.
  • given subcutaneously.
24
Q

what is mepolizumab and reslizumab? whats is its MOA?

A
  • asthma drug.
  • monoclonal antibody that bind to IL-5 which is responsible for recruitment of eosinophils.
  • used to treat eosinophilic asthma.
25
Q

MOA of H1 receptors antagonist

A
  • Gq protein linked (phosphlipase C)
  • H1 receptors increase Ca2+ concentration and activation of protein kinase C
  • H1 receptor antagonist will inhibit this action
26
Q

Cinarizine, cyclizine and promethazine are?

A
  • H1 receptor antagonist

- effective against nausea and vomiting due to motion sickness

27
Q

Muscarinic receptor antagonists and what are they used for?

A
  • hyoscine (scopolamine)

- used for the prophylaxis and treatment of motion sickness

28
Q

Adverse effects of muscarinic receptor antagonists

A
  • adverse effects include dry mouth, and blurred vision

- may also cause drowsiness

29
Q

Nabilone

A
  • synthetic cannabinol

- antagonised via naloxone (opioid receptors)

30
Q

Aprepitant/fosaprepitant

A
  • antagonist of substance P receptors (NK1 receptors) in the CTZ
  • fosaprepitant is a prodrug of aprepitant
31
Q

Dexamethasone

A
  • high doses can prevent vomiting caused by cytotoxic drugs

- MOA unknown

32
Q

what is ipratropium used for?

A
  • asthma/ COPD drug.

- anti-cholinergic which blocks secretion of Ach and causes bronchodilation.

33
Q

what is roflumilast and what is the MOA?

A
  • COPD drug

- acts by inhibiting the phosphodiesterase 4 which reduces inflammation.

34
Q

what class of drugs are cimetidine, ranitidine, nizatidine, famotidine? whats their MOA?

A
  • they are antisecretory agents, H2 antagonists used for inhibition of acid secretion in GERD.
  • H2 is a Gs, antagonizing h2 receptors decreases cAMP and therefore less acid will be released from the parietal cells because there will be less histamine.
  • it reduces both histamine and gastrin-induced acid secretion.
35
Q

what are some adverse effects of H2 antagonists (eg: ranitidine, cimetidine)

A
  • decrease in sexual function in med (in cimetidine only), galactorrhea, gynaecomastia and thrombocytopenia.
36
Q

what class of drugs are omeprazole, esomeprazole, lansoprazole, pantoprazole? and whats their MOA?

A

they are antisecretory proton pump inhibitors that are used for GERD.

  • they are WEAK BASES.
  • bind to proton pump IRREVERSIBLY and reduce the amount of H+ pumped into the stomach lumen.
37
Q

what are some side effects of proton pump inhibitors? (omeprazole)

A
  • hypergastrinemia (the body will respond by making more acid).
38
Q

what is misoprostol? MOA?

A
  • its an oral stable analogue of prostaglandin E1.
  • acts directly on ECL cells to inhibit both basal and food induced gastric acid secretion via prostaglandin EP2/3 receptor.
  • may also contribute to maintenance of mucosal barrier (leads to stimulation of mucin (EP4 receptor) and bicarbonate (EP1/2 receptor).
39
Q

whats is the side effect of using misoprostol?

A

uterine contractions- should be avoided in pregnancy

40
Q

what class of drugs are magnesium salts and aluminum salts?

A

antacids. used to neutralize acid secretion in the stomach.

41
Q

what are 2 antacids that are used for GERD?

A
  • magnesium salts and aluminum salts.
42
Q

what are some side effects of magnesium hydroxide (magnesium chloride in the stomach) and aluminum hydroxide (aluminum chloride in the stomach)?

A
  • magnesium hydroxide causes diarrhea and aluminum hydroxide causes constipation.
43
Q

what can antacids/buffers be prescribed with to prevent bloating?

A

simeticone.

44
Q

what class of drugs is bismuth chelate in terms of GERD and whats the MOA?

A
  • protectant of the mucosa
  • has toxic effects on bacillus and may prevent adherence of H.Pylori to gastric mucosa.
  • forms protective barrier over the ulcer and enhances secretion of prostaglandins, mucus and bicarbonate.
  • inhibit bacterial proteolytic enzymes.
45
Q

what are some adverse effects when it comes to bismuth chelate?

A
  • blackening of the tongue and feces
  • tinnitus
  • can result in encephalopathy (Reye’s syndrome) if renal excretion is impaired)
46
Q

what is Sucralfate and what is the MOA?

A
  • protects the mucosa for GERD
  • its a complex aluminium hydroxide and sulfated sucrose that forms a viscous paste in the acidic media
  • it binds positively charged proteins in the ulcer forming a protective barrier
  • reduces degradation of mucus via pepsin
  • can stimulate secretion of mucous, bicarbonate and prostaglandins from the gastric mucosa.
47
Q

what are some antibiotics used to treat H.pylori?

A

amoxicillin, metronidazole, clarithromycin, tetracycline.

PharmacologyII (12 decks)

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