الحلقة 5 من كورس كلنيكال فارما (من جزء الجهاز العصبي اللاإرادي)

Nicotinic Agonists ( Ganglion stimulant )

NN Adrenal medulla, CNS and Autonomic ganglia (Symp. and parasympathetic).

NM Neuromuscular junction (NMJ).

Nicotine (Nicorette®)

- Nicotine activate nicotinic receptors in small dose (large dose act as blocker effect).

- Nicorette® products (chewing gum, lozenges, patches oral spray inhalator, sublingual

tablets and nasal spray) aid in smoking cessation.

- Stimulate nicotinic receptor on both sympathetic and parasympathetic.

 Sympathetic stimulation increase adrenaline and nor-adrenaline release

increase cardiac force increase cardiac output (CO) → VC Increase blood

pressure (BP).

 Parasympathetic stimulation increase motility and all secretion.

Varenicline (Chantix®)(Champix®)

Chantix® in the USA and Champix® in Canada Europe and other countries.

Varenicline is an oral drug used to quit smoking.

- Act as a partial agonist in the nicotinic receptors partially stimulates the receptors without

producing a full effect like nicotine.

Dose - Days 1 to 3  0.5 mg orally once a day.

- Days 4 to 7  0.5 mg orally twice a day.

- Days 8 to end of treatment 1 mg orally twice a day.

* Patients should be treated with varenicline for 12 weeks.

- Most common adverse effects Nausea, vomiting. headache, constipation, sleep disturbance

and unusual dreams.

-Varenicline are contraindicated in pregnancy (category C).

- In 2007, the FDA received post-marketing reports of thoughts of suicide in people using

varenicline.

- In 2009, the FDA requires varenicline to carry a black box warning that the drug should be

stopped if suicidal behavior are developed.

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