Nifedipine sublingual

Nifedipine (Table 3) is a potent vasodilator that selectively dilates resistance vessels and has fewer effects on venous vessels. It does not cause reflex tachycardia during chronic therapy. Nifedipine is one of the first-line choices for black or elderly patients and patients having concomitant angina pectoris, diabetes, or peripheral vascular diseases. Nifedipine, sublingually, is also suitable for the treatment of hypertensive emergencies. Nifedipine does not impair sexual function or worsen blood Hpid profile. The side effects are flushing, headache, and dizziness. 

Patients with malignant-accelerated hypertension can usually be managed by oral therapy. Patients who are seen in a nursing home or clinic, whose BP is found to be above some arbitrary danger level like a BP of 180/120 should not automatically be given nifedipine sublingually. Indiscriminate use of nifedipine sublingually could lead to a major catastrophe like myocardial infarction or cerebrovascular episodes. Nifedipine activates sympathetic response and leads to precipitous drops of blood pressure followed by rebound hypertension. 

For patients who have difficulty swallowing dilti-azem, tablets can be crushed and mixed with food or liquids. However, the patient should swallow the sus-tained-released tablets whole and not chew or divide them. When nifedipine is ordered sublingually, the capsule is punctured with a sterile needle and the liquid squeezed under the tongue or in the buccal pouch. 

Nifedipine is associated with fewer side effects than magnesium or ft-agonist therapy. Five to 10 mg nifedipine may be administered sublingually every 15 to 20 minutes for three doses. Once stabilized, 10 to 20 mg may be administered by mouth every 4 to 6 hours for preterm contractions. 

Drugs for the control of hypertensive crises include nifedipine (capsule, to be chewed and swallowed), nitroglycerin (sublingually), clonidine (p.o. or i.v., p. 96), dihydralazine (i.v.), diazoxide (i.v.), fenoldopam (by infusion, p. 114) and sodium nitroprusside (p. 120, by infusion). The nonselective a-blocker phentolamine (p. 90) is indicated only in pheochromocytoma... 

Self-medication of a MAOI-induced hypertensive crisis is controversial. In a hypertensive crisis the lack of access to medical services may lead to even greater complications. A small dose of medication taken as part of a larger plan to blunt the rise in blood pressure may prevent serious complications. However, headache is common, has multiple causes, and patients may not accurately identify a headache due to hypertension without a blood pressure check. In addition, selfadministration of nifedipine, especially sublingually, may result in needless and perhaps dangerous drops in blood pressure. 

Clary C, Schweizer E Treatment of MAOl hypertensive crisis with sublingual nifedipine. J Cbn Psychiatry 48 249-250, 1987... 

The sublingual surface area is relatively small but has a rich blood supply. The major advantage of this route is avoidance of intestinal destruction and hepatic first pass metabolism. However, absorption can be highly variable critical factors are the residence time of the drug in the mouth and saliva flow. Premature swallowing or excessive saliva production preclude efficient absorption. Nitroglycerin, nifedipine, propranolol, and buprenorphine are all available as sublingual preparations. Rectal... 

Pereira et al. (1993) evaluated postoperative pain relief and incidence of side-effects of the combination of epidural morphine (0.5 mg) and sublingual nifedipine (10 mg). In this double-blind, placebo-controlled study 36 women were submitted to elective operations (hysterectomy and colpoperineoplasty). The nifedipine-treated group showed a significant drop in blood pressure which was controlled by rehydration. The results indicate that epidural morphine-induced postoperative pain relief may be enhanced by systemic administration of nifedipine with easily controlled side-effects. 

Save, T., et al. 1994. Comparative study of buccoadhesive formulations and sublingual capsules of nifedipine. J Pharm Pharmacol 46 192. 

Nifedipine 45-70% < 1 minute (IV), 5-20 minutes (sublingual or oral) 4 About 90% bound to plasma protein metabolized to an acid lactate. 80% of the drug and metabolites excreted in urine. 

Labetalol can be given orally or intravenously. Nifedipine can be given orally in general the SR preparation is used and it is never used sublingually so as not to drop the blood pressure too quickly. 

Single oral or sublingual dose of a calcium channel blocker (e.g., nifedipine) for urgent treatment of hypertension due to drug interaction or dietary tyramine... 

For immediate pre-exertional prophylaxis glyceryl trinitrate sublingually or nifedipine (bite the capsule and hold the liquid in the mouth or swallow it). 

Dijfuse oesophageal spasm may be helped by isosorbide dinitrate 5 mg sublingually or 10 mg by mouth, or by nifedipine 10 mg sublingually or swallowed. 

Compounds that are currently marketed or are being considered for buccal or sublingual routes include organic nitrates, barbiturates, papaverine, trypsin, prochlorperazine, benzodiazepines, buprenorphine, capto-pril, isoprenalin, oxytocin, and nifedipine. Oxytocin is currently the only peptide marketed in sublingual form. Sublingual steroids have been examined with moderate success. 

In the past, the difficulties presented in the administration of drugs in the treatment of hypertensive emergencies were largely overcome with the use of nifedipine administered sublingually. The onset of action was rapid, and the drug was also used sublingually for the treatment of acute attacks of angina pectoris. Presently, two types of formulation of nifedipine are available, both intended primarily for peroral administration. The sustained-release formulation is... 

Hauger-Klevene, J.H. Comparison of sublingual captopril and nifedipine. Lancet 1986, 1, 219. 

Zangerle BIF, Wolford R. Syncope and conduction disturbances following sublingual nifedipine for hypertension. Ann Emerg Med 1985 14(10) 1005-6. 

Shettigar UR, Loungani R. Adverse effects of sublingual nifedipine in acute myocardial infarction. Crit Care Med 1989 17(2) 196-7. 

Sublingual nifedipine, given for hypertensive crises in elderly patients, can cause adverse effects associated with a precipitous fall in blood pressure, even at low doses. In 93 consecutive hypertensive patients without coronary heart disease, aged 65 years or over, nifedipine reduced blood pressure significantly, increased heart rate, and relieved sjmptoms associated with raised blood pressure (9). However, there were electrocardiographic changes consistent with myocardial ischemia in six of 55 patients with left ventricular hypertrophy and in one patient without left ventricular hypertrophy. 

Rapid lowering of the blood pressure with nifedipine, particularly sublingually, can precipitate cerebral ischemia, with confusion, loss of consciousness, and stroke. Cases of cortical blindness with macular sparing secondary to occipital lobe infarction have been reported (SEDA-17, 238). 

Transient cerebral ischemia, with aphasia and hemipar-esis in one patient and cerebellar dysfunction and loss of consciousness in another, has been observed with nifedipine (12). In addition, rapidly progressive hemiparesis, aphasia, and confusion, accompanied by a substantial fall in blood pressure, occurred in a patient whose hypertension (230/136 mmHg) was treated with sublingual nifedipine (13). Transient retinal ischemia, which may be recurrent, has also been attributed to nifedipine (14,15). Hypotension or cerebral steal are the likely mechanisms. 

Ishibashi Y, Shimada T, Yoshitomi H, Sano K, Oyake N, Umeno T, Sakane T, Murakami Y, Morioka S. Sublingual nifedipine in elderly patients even a low dose induces myocardial ischaemia. Clin Exp Pharmacol Physiol 1999 26(5-6) 404-10. 

Ellrodt AG, Ault MJ, Riedinger MS, Murata GH. Efficacy and safety of sublingual nifedipine in hypertensive emergencies. Am J Med 1985 79(4A) 19-25. 

Pedro-Botet J, Minguez S, Supervia A. Sublingual nifedipine-induced anaphylaxis. Arch Intern Med 1998 158(12) 1379. 

Silfvast T, Kinnunen A, Varpula T. Laryngeal oedema after isosorbide dinitrate spray and sublingual nifedipine. 

Similar topical formulations containing steroids, antibiotics and antimycotics are described in patents [468,469]. Nifedipine is an example of a drug that is used in sublingual sprays with copovidone [468]. 

Nifedipine ( Adalat, Bayer 10A0)(20), used for the treatment of angina, 87 is a powerful peripheral vasodilator and has hypotensive properties in man.88 A dose of 30mg sublingually lowered blood pressure substantially in 1A essential hypertensives for more than k hrs. with a rise in heart rate and plasma renin activity. Nifedipine interferes with the transmembrane calcium flux causing a reduction in vascular smooth muscle tone.87)89 The conformational requirement for dopamine induced renal... 

Oral or sublingual immediate-release nifedipine has been used in the office setting, nursing homes, and hospitals for acute BP lowering but is potentially dangerous. This approach produces a rapid reduction in BP. Immediate-release nifedipine should never be used for hypertensive urgencies because of reports of severe adverse events such as myocardial infarctions and strokes. ... 

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