1.1 glyceryl trinitrate GTN

class

organic nitrate vasodilator

indication

used in acute managment/prevention of angina pectoris + heart failure

mechanism of action

• GTN releases nitric oxide, NO → relaxes vascular smooth muscle

• NO activates guanylyl cyclase increasing cyclic GMP levels

• results in vasodilation thus reducing myocardial oxygen demand and improving blood flow

GTN SL tablets rational for use

immediate absorption into blood stream + ensures rapid relief of symptoms

avoids hepatic first pass metabolism enhancing bioavailability

GTN SL tablet forms + onset action

available as sublingual tablets/ sprays

onset withing 1-3 minutes with effects lasting 30 min -1 hour

GTN SL tablets usage instructions

place tablet under the tounge and let is dissolve without swallowing

avoid eating or drinking until tablet is fully dissolved

GTN SL tablets side effects

common= headache + dizziness + flushing

serious= hypOtention, when combined with phosphodiesterase inhibitors (sildenafil)

formulation design

disintegration

taste masking agents

adhesive polymers

buffers

disintegrants

aid rapid dissolution

taste masking agents

improve patient compliance

adhesive polymers

prolong retention for buccal tablets

buffers

maintain optimal pH for drug stability + absorption