[KLOHnihdeen Pregnancy Category C

Apo-Clonidine M; Catapres; Cat-apres-TTS-1, -2, and -3; Dixarit M; Du-raclon, Novo-Clonidine M, Nu-Clonidine M [Rx]

Classification: Antihypertensive, centrally acting antiadrenergic

See also Antihypertensive Agents. Action/Kinetics: Stimulates alpha-adrenergic receptors of the CNS, which results in inhibition of the sympathetic vasomotor centers and decreased nerve impulses. Thus, bradycardia and a fall in both SBP and DBP occur. Plasma renin levels are decreased, while peripheral venous pressure remains unchanged. Few orthostatic effects. Although NaCl excretion is markedly decreased, potassium excretion remains unchanged. Tolerance to the drug may develop. Onset, PO: 30-60 min; transdermal: 2-3 days. Peak plasma levels, PO: 3-5 hr; transdermal: 2-3 days. Maximum effect, PO: 2-4 hr. Duration, PO: 12-24 hr; transdermal: 7 days (with system in place). tV2: 12-16 hr. Approximately 50% excreted unchanged in the urine; 20% excreted through the feces.

The transdermal dosage form contains the following levels of drug: Catapres-TTS-1 contains 2.5 mg clonidine (surface area 3.5 cm2), with 0.1 mg released daily; Catapres-TTS-2 contains 5 mg clonidine (surface area 7 cm2), with 0.2 mg released daily; and Catapres-TTS-3 contains 7.5 mg clonidine (surface area 10.5 cm2), with 0.3 mg released daily.

Epidural use causes analgesia at presynaptic and postjunctional al-pha-2-adrenergic receptors in the spinal cord due to prevention of pain signal transmission to the brain. tv2, distribution, epidural: 19 min; elimination: 22 hr. Uses: Oral, Transdermal: Mild to moderate hypertension. A diuretic or other antihypertensive drugs, or both, are often used concomitantly. Non-FDA Approved Uses: Alcohol withdrawal, atrial fibrillation, attention deficit hyperactivity disorder, constitutional growth delay in children, cyclosporine-associated nephro-toxicity, diabetic diarrhea, Gilles de la Tourette's syndrome, hyperhidrosis, hypertensive emergencies, mania, menopausal flushing, opiate detoxification, diagnosis of pheochromocy-toma, postherpetic neuralgia, psychosis in schizophrenia, reduce allergen-induced inflammatory reactions in extrinsic asthma, restless leg syndrome, facilitate smoking cessation, ulcerative colitis.

Epidural: With opiates for severe pain in cancer clients not relieved by opiate analgesics alone. Most effective for neuropathic pain. Contraindications: Hypersensitiv-ity to the drug or its components. Special Concerns: Use with caution in presence of severe coronary insufficiency, recent MI, cerebrovascu-lar disease, or chronic renal failure. Use with caution during lactation. Safe use in children not established. Geriatric clients may be more sensitive to the hypotensive effects; a decreased dosage may also be necessary in these clients due to age-related decreases in renal function. For children, restrict epidural use to severe intractable pain from malignancy that is not responsive to epidural or spinal opiates or other analgesic approaches.

Side Effects: CNS: Drowsiness (common), sedation, confusion, diz-

■ ziness, headache, fatigue, malaise, nightmares, nervousness, restlessness, anxiety, mental depression, increased dreaming, insomnia, hallucinations, delirium, agitation. Oral: Dry mouth (common), taste changes. GI: Constipation, anorexia, N&V, parotid pain, weight gain, hepatitis, parotitis, ileus, pseudo-obstruction, abdominal pain. CV: CHF, severe hypotension, Raynaud's phenomenon, abnormalities in ECG, palpitations, tachycardia and bradycardia, postural hypotension, conduction disturbances, sinus bradycardia, CVA. Dermatologic: Urticaria, skin rashes, sweating, angioneurotic edema, pruritus, thinning of hair, alopecia, skin ulcer. GU: Impotence, urinary retention, decreased sexual activity, loss of libido, nocturia, difficulty in urination, UTI. Respiratory: Hypoventilation, dyspnea. Musculoskeletal: Muscle or joint pain, leg cramps, weakness. Other: Gynecomastia, increase in blood glucose (transient), increased sensitivity to alcohol, chest pain, tinnitus, hyperaesthesia, pain, infection, thrombocytopenia, syncope, blurred vision, withdrawal syndrome, dryness of mucous membranes of nose; itching, burning, dryness of eyes; skin pallor, fever.

Transdermal products: Localized skin reactions, pruritus, erythema, allergic contact sensitization and contact dermatitis, localized vesicula-tion, hyperpigmentation, edema, excoriation, burning, papules, throbbing, blanching, generalized macular rash.

NOTE: Rebound hypertension may be manifested if clonidine is withdrawn abruptly.

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