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Medical Pharmacology of Derm, Gastro and Pallitive Care
Questions regarding the medical pharmacology of dermatology, gastroenterology and palliative care (focusing on pain)
44
Medical
Undergraduate 3
08/07/2013

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Cards

Term
What are two examples of 5-ASA drugs?
Definition
Olsalazine, Mesalazine
Term
What is the MoA of 5-ASAs?
Definition
Acts locally to decrease inflammation in the colon by inhibiting prostaglandin formation.
Term
Compare and contrast 5-ASAs and Sulfasalazine.
Definition

Sulfasalazine contains a 5-ASA and a sulfapyridine.  The sulfapyridine is responsible for producing AEs: headaches, nausea, rasha, reversible infertility, malaise, gas and cramps. (still seen in 5-ASA)

 

Sulfasalazine is indicated only in RA now, as 5-ASA have surpassed it.

Term
Olsalazine is indicated in?
Definition

The treatment of chronic IBD.  Including inducing and maintaining remission in mild UC.

 

They are less effective in Crohns.

Term
What kind of pathogenic bacteria are most frequently found in the GIT? Which antibiotic is most effective against these?
Definition

Gram negative obligate anaerobes are the most likely bacteria. 

 

Metronidazole is an effective antibiotic against these bacteria. Alcohol is contraindicated in metronidazole use.

Term
Describe the triple antibiotic therapy of the GIT?
Definition
Gentamicin, Ampicillin and Metronidazole
Term
This class of drug is cytotoxic and frequently cause blood dyscrasias.  They are effective antiinflammatories.
Definition
DMARDs: Disease Modifying Anti Rheumatoid Drugs.  Originally designed specifically for RA, they are used in a number of autoimmune mediated inflammatory diseases. i.e. IDB
Term
What are the common DMARDS?  What is their main advantage in inflammatory conditions?
Definition

Methotrexate (purine inhibition), Ciclosporin (calcineurin inihibitor), Azathioprine (purine),

Monoclonal Ab- Adalimumab, Inflixumab TNF alpha inihibitors

Chloroquine and hydrochloroquine (IL suppression)

 

There biggest advantage is that they are steroid sparing

Term
Describe the typical treatment plan for mild UC?
Definition

Many patients receive an NSAID and at least one DMARD, sometimes with low-dose oral glucocorticoids. If disease remission is observed, regular NSAIDs or glucocorticoid treatment may no longer be needed.

Term
The most common NSAIDs are?
Definition
Aspirin, Ibuprofen and Naproxen
Term
The most common issues surrounding long-term NSAID use are?
Definition
Renal impairment (constrict afferent arterioles and decrease GFR) and GIT ulceration (leading to hemorrhage and perforation)
Term
First line therapy for UC is?
Definition
Mesalazine - a 5-ASA anti-inflammatory
Term
DMARD use can cause a number of AEs, most notable among which is?
Definition
immunosuppression predisposing to infection
Term
Antidiarrheal drugs are any medications that provide symptomatic relief from diarrhea.  Give three different mechanisms used to achieve this?
Definition
Fluid and electrolyte replacement, bulking agents, absorbants, anti-inflammatories and opioids.
Term
What is bismuth-subsalicylate?
Definition

It is a combination antacid/antidiarrheal.  It reduces the secretion of fluid into the gut and increases absorption.

 

It may cause black tongue and black stool.

Term
The mechanism of action of the opioid family?  Common side effects?
Definition

Opioids work as mu receptor agonists against pain and diarrhea.

 

The common side effects are respiratory depression, sedation, constipation and euphoria.

Term
Loperamide is an opioid used to treat diarrhea.  How does it do this?
Definition

It is an opioid receptor agonist in the myenteric plexus, decreasing the activity of the ircular smooth muscle.

 

It is contraindicated in compromised hepatic patient.

Term
Hepatic encephalopathy is a serious acute exacerbation of hepatic disease.  Management includes?
Definition
Lactulose.  Lactulose draws out the excess ammonium that causes injury in hepatic encephalopathy.
Term
The 7 steps in the management of constipation are?
Definition
  1. Exercise and diet - fibre
  2. Bulking agents - Metamusil
  3. Stool softner - Coloxyl
  4. Osmotic laxatives - Movicol
  5. Stimulants - Coloxyl and Senna
  6. Suppositories - Duracol
  7. Lavage 
Term
What are the two components to Sennoside and how do they work?
Definition

Coloxyl draws water into the colon to soften the stool

Senna increases muscle activity to move the stool

Term
What kind of agent is Metoclopromide and when is it indicted?
Definition

Metoclopromide is an antiemetic and a gastro prokinetic.  It is a dopamine antagonist.  It is used to treat constipation and nausea.

It is the most common cause of drug induced movement disorders i.e tardive dyskinesia

Term
Compare and contrast Prochlorperazine and Ondansetron?
Definition

Prochlorperazine is an extremely strong typical antipsychotic (dopamine antagonist) indicated in resistant nausea and vomiting.  It has significant EPSE.  Particularly post chem/radio therapy. 5-10 minute onset and 4 hr action.

 

Ondansetron is a 5-HT serotonin antagonist indicated particularly in post chemotherapy nausea and vomiting.  Ondansetron is a well tolerated drug with few side effects.  It is very expensive.

 

Term
In what situation is Methylnaltrexone indicated?
Definition
Methylnaltrexone reverses the peripheral action of opioid agonists, treating the opioid induced symptoms of constipation and withdrawal whilst preseving analgesia.
Term
Opioid overdose presents as a typical toxidrome with respiratory depression, coma and pin point pupils.  How do we reverse this syndrome?
Definition
Naloxone reverses the effects of opioids.  It is a competitive antagonist.
Term
The gold standard for mono-pharmacy antiemetic is?
Definition
Levomepromazine: it is a dopamine antagonist, is very effective and has a minor analgesic effect as well.
Term
Give three examples of antiemetics which work in different ways?
Definition
Haloperidol, metoclopramide and promethazine
Term
Hyoscine is an anticholinergic, how does it work and an antiemetic?  When is it indicated over other antiemetics?
Definition
As an anticholinergic it decreases bowel activity as well as this it decreases secretions making it very effective in apparent bowel obstruction.
Term
Which corticosteroid is effective in sub-acute bowel obstruction?
Definition
Dexamethasone, it also has an antiemetic action.
Term
Is hydromorphone more or less potent than morphine?
Definition
Hydromorphone is 7x more potent than morphine.
Term
Advantages and disadvantages of hydromorphone?
Definition

It has less cognitive impairment i.e. good in elderly

Produces neurotoxic metabolites

 

Term
Compare and contrast fentanyl and oxycodone?
Definition

Fentanyl is a potent, synthetic opioid analgesic with a rapid onset and short duration of action.  It is indicated for breakthrough pain and can be administered transdermally.  Safest opioid.


Oxycodone s a narcotic analgesic generally indicated for relief of moderate to severe pain.  Second line to morphine for cancer pain.  High risk of addiction and withdrawal symptoms.

Term
Mechanism of action of Ketamin and indication?
Definition
Ketamine is an NMDA antagonist used for neuropathic pain.
Term
What is the main injectable NSAID? Advantages/ Disadvantages?
Definition
Ketoralac: is an injectable NSAID.  It is opioid sparing and effective in bone pain.  High risk of ulceration.
Term
What is the advantage of applying medication directly to the affected tissue?
Definition
Avoid systemic circulation
Term
The four factors that affect penetration of medication are?
Definition
Vehicle, age, permeability and hydration
Term
Are water soluble drugs delivered more effectively in gels or ointments?
Definition
Gels, high water content.
Term
Are lipid soluble drugs delivered more effectively in gels or ointments?
Definition
Ointments
Term
Give three examples of vehicles?
Definition
Gel, Lotion, Paste, Cream, Paint, Dust, Ointment
Term
What is the general MoA of topical corticosteroids?
Definition
Antiinflammatory, immunosuppresive and importantly vasoconstrictive action.
Term
Is hydrocortisone the weakest or strongest corticosteroid? Give another example?
Definition

Hydrocortisone is the weakest topical corticosteroid.

Betamethasone is much stronger.

Term
Describe the most effective administration plan for corticosteroids, why?
Definition

Corticosteroids should be deliever in pulses, using the most potent preparation possible for the shortest amount of time.

 

Occlusion of site can help concentrate medication.

Term
The local adverse effects of steroids? The systemic affects?
Definition

Epidermal atrophy, striae, hypopigmentation

Hyperglycemia, immunosuppresion, adrenosuppression and Cushing's syndrome.

Term
Efudex (5FU) MoA & is used to treat?  The patient needs to know that?
Definition

Inhibitis DNA synthesis of fast growing dysplastic cells.  

Is used to treat solar keratosis.  

3-5 days reddening --> 2 weeks of blistering --> 4 weeks of erosion.

Term
What is imiquimod and how does it work?
Definition

Indicated in the treatment of superficial BCC or SK on the face and genitals.  

It induces infiltration of tumor destructuve cells. 

Poor compliance due to specific instructions.

Very few systemic symptoms.

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