Clonidine

Clonidine

1. CLONIDINE BY ABBAS FADHIL 1

2. CLONIDINE Clonidine. Category adrenergic α 2 receptor . The treatment of hypertension. (trade names_ Catapres , Kapvay , Nexiclon , Clophelin ) Formula C 9 H 9 Cl 2 N 3 2

3. α 2-RECEPTOR The Alpha2  Adrenergic Receptor  is an inhibitory G-protien coupled receptor that binds  norepinephrine  and is present in both the CNS and sympathetic arm of the ANS. Within  sympathetic  fibers, Alpha2 receptors are uniquely found on the  presynaptic  terminals of postganglionic. 3

4. presynaptic postsynaptic 4

5. Mechanism of action Clonidine treats high blood pressure by stimulating α2 receptors in the brain, thus inhibiting the release of norepinephrine (NE). And then decreases peripheral vascular resistance, will become vasodilation and the pressure will decrease. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. 5

6. The α-2 receptors constitute a family of G-protein–coupled receptors with 3 pharmacological subtypes, α-2A, α-2B, and α-2C . The α-2A and -2C subtypes are found mainly in the central nervous system. Stimulation of these receptor subtypes may be responsible for sedation, analgesia. 6

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8. Pharmacokinetics Bioavailability: Immediate release (75-85 %) Protein bound: 20-40% Duration : 6-10 hr. Metabolism in Liver. Elimination Half-life : 12-16 hr. Excretion: Urine. 8

9. CLONIDINE MEDICAL USED Hypertension severe dysmenorrhea vascular migraine headaches treatment of alcohol withdrawal used in conjunction with benzodiazepines. 9

10. attention-deficit hyperactivity disorder (ADHD) Restless Legs Syndrome Tourette's Syndrome 10

11. 8-Epidural clonidine analgesia for cancer pain. 11

12. DOSAGE FORM ORAL TABLET 0.1mg 0.2mg 0.3mg 12 2 times a day (morning and bedtime ) to 0.1 mg

13. injectable solution:- 100mcg/ml 500mcg/ml 13

14. 3.Transdermal patch, 0.1mg/day 0.2mg/day 0.3mg/day 14 Change every 7 days

15. Side effect Very common side effects is:- Dizziness Skin reactions (if given transdermally ) Orthostatic Somnolence (dose-dependent ) 15

16. Common side effects:- Constipation vomiting Rash Weight gain/loss 16

17. Rare side effects:- Hallucination Pruritus Nasal dryness Alopecia 17

18. Clonidine and Pregnancy Pregnancy Category C. Clonidine may be pass through the barrier of placenta then enter blood circulation of fetus and cause decrease blood pressure of the fetus with decrease heart rate. May be die. Clonidine can pass into breast milk and may harm the baby; caution is warranted in women who are pregnant, planning to become pregnant, or are breastfeeding. 18

19. 19 FDA PREGNANCY CATEGORY

20. Interaction Drug interactions may change how your medications work or increase your risk for serious side effects . Do not start, stop, or change the dosage of any medicines without your doctor's approval. Interaction 20

21. Aspirin:- Using aspirin with clonidine may increase side effects such as dizziness, drowsiness, confusion, and difficulty concentrating . Atenolol:- clonidine, atenolol. Either increases toxicity of the other by unspecified interaction mechanism. Avoid or Use Alternate Drug. Can increase risk of bradycardia . Clomipramine:- This combination may cause vomiting, sweating, flushing, dizziness, headache or heart palpitations. 21

22. Interaction With Food Ginseng:  Clonidine is used in the treatment of hypertension. Interaction of clonidine with ginseng may affect the action of the drug as ginseng can increase the blood pressure . Other Herbs:  Saw palmetto, hawthorn, goldenseal, licorice and yohimbe may increase the blood pressure and interfere with the effect of clonidine.  22

23. The End Thank 4 you 23

24. 24 REFERENCE www.drugs.com www.uspharmacist.com http:// www.pathwaymedicine.org www.webmd.com www.medscape.com www.drugbank.ca http:// www.medicalook.com www.wikipedia.org www.healthline.com www.medindia.net