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Pharm407 > Lecture 4 part 2: Pharmaceutical aspects of CVD1 > Flashcards

Lecture 4 part 2: Pharmaceutical aspects of CVD1 Flashcards

1
Q

What are the two types of nitrates available in NZ?

A

Glyceryl trinitrate

Isosorbide mononitrate

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2
Q

What are the characteristics of GTN? (2 points)

A
  • explosive when pure (also known as nitroglycerin)

- unpredictable and low oral bioavailability

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3
Q

What are the characteristics of isosorbide mononitrate? (1 point)

A

-good oral bioavailability

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4
Q

What was the mainstay treatment for angina prior to 1857? (1 point)

A

-patients were bled to relieve angina pain.

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5
Q

How were nitrates discovered? (4 points)

A
  • Prior to 1857, Brunton noticed that administration of inhaled amyl nitrate relieved angina in 30-60 seconds
  • in 1846 Sobero noticed a small amount of GTN under the tongue caused a headache
  • In the late 1860s, Nobel’s dynamite factories manufactured GTN. Workers developed headaches at the start of the week which were relieved by weekends.
  • workers with angina noticed reduction in chest pain on mondays but this returned in the weekend
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6
Q

What are the indications for nitrates that should be considered? (3 points)

A
  • Time till onset of action
  • duration of effect
  • extended release.
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7
Q

What are the ideal properties of nitrates for symptomatic relief?

A

-Fast onset to relieve sudden symptoms of angina e.g. GTN spray

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8
Q

What are the ideal properties of nitrates for regular use?

A
  • Long duration of action so that we can use it prophylactically and have effect over a long period of time (e.g. GTN patch)
  • A release of drug which is sustained and doesnt fluctuate too much in concentration (e.g. Duride CR tablets)
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9
Q

Why are CR Duride tablets 6 hours long when CR Blood pressure tablets which are CR over 24 hours? (3 points)

A
  • If someone is taking nitrate regularly, they may develop tolerance unless there is a nitrate free period (8-12 hours long)
  • If this period is not nitrate free, the patient may not experience relief with the GTN if they get angina due to build up of tolerance
  • Duride CR is formulated over a shorter period of time to allow for this nitrate free period.
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10
Q

What are the mechanisms of nitrate tolerance? (5 points)

A
  • Increased reactive oxygen species
  • increased plasma volume
  • decreased biotransformation of nitrates to NO
  • decreased responsiveness to NO
  • neurohormonal activation
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11
Q

When is nitrate tolerance lost?

A

-within 24 hours of discontinued therapy

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12
Q

What are the list of nitrate formulations available in NZ? (7 points)

A
  • SL spray (Nitrolingual)
  • SL tablets (Lycinate)
  • solution for injection (Nitronal)
  • transdermal patch (Nitroderm)
  • immediate release tablets (Ismo20)
  • modified release tablets (Duride)
  • rectal ointment (Rectogesic for anal fissures)
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13
Q

What are the PK properties of the GTN spray? (5 points)

A
  • 0.4mg GTN/spray
  • Tmax = 4 minutes
  • Half life = 2.5-4.5 minutes
  • metabolites less active than parent compound
  • Shelf life = a few years.
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14
Q

What are the PK properties of Lycinate tablets? (4 points)

A
  • Releases 0.6mg of GTN/tablet
  • Tablet dissolves under the tongue
  • Tmax = 4.9 minutes
  • Shelf life = 8 weeks from opening (difficult as 1 bottle = 100 tablets)
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15
Q

What are the PK propeties of Nitronal solution for IV administration? (5 points)

A
  • 1mg/mL clear aqueous solution
  • Isotonic
  • Tmx = immediate
  • bioavailability = 100%
  • has definied protocols for use
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16
Q

What are the differences between Nitroderm TTS 5 and Nitroderm TTS 10? (2 points)

A
  • Nitroderm TTS 5 delivers 25mg of drug while TTS 10 delivers 50m of drug
  • TTS 5 has a smaller drug releasing area of 10 cm^2 while TTS 10 has a bigger drug releasing area of 20 cm^2
17
Q

What are the PK properties of Nitroderm? (6 points)

A
  • Releases 20-25ug/cm^2/hour
  • TTS 5 and 10 numbers denote the amount of active drug released over 24 hours
  • can be applied to upper arm, trunk, chest
  • Plasma levels plateau after 2 hours
  • Plasma levels proportional to area available for drug release to skin
  • Patch cannot be halved!
18
Q

Why is there such a high concentration of drug in a nitroderm TTS if a nitrate free period is needed?

A

-A high concentration in the patch drives the concentration of the drug into the skin (drug moves from high concentration to low concentration)

19
Q

What are the PK properties for Ismo 20? (6 points)

A
  • Conventional release tablets which deliver 20mg isosorbide mononitrate
  • Release is governed by elements of NW equation
  • Bioavailabiltiy ~ 100%
  • Onset of action = 20 min
  • Tmax = 1 hour
  • Half life = 5 hours
  • usual dose = 20mg bd/tds
20
Q

What are the PK properties of duride tablets? (6 points)

A
  • MR tablets which deliver 60mg isosorbide mononitrate
  • drug released independent of pH over 10 hours. Produces clinical effect of 12 hours
  • Bioavailability = 90%
  • T max = 4 hours
  • Half life = 5 hours
  • Can be divided but not crushed or chewed.
21
Q

How does the MR formulation of Duride work? (2 points)

A
  • The drug is dispersed in a polymer

- Over time the drug diffuses out, leaving a ghost polymer which is excreted in the faeces.

22
Q

What is the significance of pH independent release of Duride over 10 hours?

A
  • Duride tablets are exposed to a range of pH as it goes through the GIT
  • pH independent release means that it will release the drug over the entire length of the GIT irregardless of environmental pH, thus producing 12 hours of clinical effect
23
Q

What is the role of a bare metal stent?

A

-Increase blood flow through an artery by preventing collapse or re-occlusion

24
Q

What are the disadvantages of bare metal stents? (3 points)

A
  • Risk of immune response and cell proliferation over stent
  • Risk of stent thrombosis
  • Antiplatelet therapy is required
25
Q

What are drug eluting stents? (2 points)

A
  • Aims to reduce immune/thrombotic response of stents

- Consists of expandable metal framework and polymer coating which releases the drug

26
Q

What are examples of drug eluting stents used in NZ? (3 points)

A
  • Xience Promus releases everolimus
  • Endeavour releases zotarolimus
  • Cypher releases sirolimus
27
Q

How does a drug eluting stent work? (5 points)

A
  • Uses non-immunogenic metal alloys
  • Polymer coating the metal stent structure provides the extended release of the drug
  • Once drug is exhausted (over 6-12 months) the polymer remains
  • Biocompatibility of polymer is of vital importance
28
Q

How is the stent placed in a diseased artery? (2 points)

A
  • A cather is inserted during PTCA. It has a stent and baloon at its tip
  • Once guided to the intended site, the stent is expanded
29
Q

What is Xience promus? (5 points)

A
  • Releases everolimus
  • Indicated for improving coronary lumina diameter in patients with coronary artery thinning
  • permanent implant
  • correct stent length and diameter must be accurately determined
  • stent must be fully expanded to ensure positionfixutre.
30
Q

What is restenosis? (3 points)

A
  • Defined as reduction of lumen diameter of 50% following intervention
  • Implanted bare metal stent reduces occurrence and severity compaired to PCTA alone
  • further improvement is shown by drug eluting stents over bare metal stents in maintaining long term patency of blood vessel
31
Q

What is tenecteplase? (5 points)

A
  • Recombinant DNA fibrin specific plasminogen activator
  • thrombolytic agent indicated for use in acute phase of MI
  • administered as single IV bolus
  • Device is designed for ease of administration
  • dose is based on body weight
32
Q

How is Tenecteplase prepared to be administered? (7 points)

A
  • open box of vial-adapter, remove tip cap from syringe and remove the flip off cap from the vial.
  • Crew pre-filled syringe on the vial adapter tightly
  • penetrate the vial stopper in the middle with the spike of the vial adapter
  • add water for injections by pushing the syringe plunger slowly down to avoid foaming
  • reconstitute by swirling gently
  • invert vial/syringe and transfer appropriate volume of solution into syringe according to dosing instructions
  • Disconnect syringe from vial adapter. Solution is ready for IV bolus injection

Pharm407 (5 decks)

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