Side Effects of Sular (nisoldipine)

Sular (nisoldipine) is a calcium channel blocker (CCB) used to treat high blood pressure (hypertension).

Calcium channel blockers prevent calcium from entering certain types of muscle cells. Since muscle cells need calcium to contract, CCBs prevent the cells from contracting, that is, they cause the muscle cells to relax.

Sular selectively relaxes the muscles of small arteries causing the arteries to dilate but has little or no effect on muscles of veins or the heart. Dilation of arteries reduces blood pressure. 

Common side effects of Sular include

• swollen ankles and feet,
• headache,
• dizziness,
• nausea,
• palpitations, and
• hypersensitivity reactions.

Serious side effects of Sular include

• worsening chest pain,
• low blood pressure, and
• heart attacks.

Drug interactions of Sular include cimetidine, ketoconazole, itraconazole, erythromycin, or any drug that reduces the activity of liver enzymes that break down Sular, because they can increase blood levels of Sular possibly causing more side effects.

The effects of Sular in pregnancy are unknown. It is unknown if Sular appears in breast milk. Consult your doctor before breastfeeding. 

The most common side effects of nisoldipine are:

• Peripheral edema (swollen ankles and feet),
• headache,
• dizziness,
• nausea,
• palpitations,
• Hypersensitivity reactions,
• worsening of chest pain,
• low blood pressure, and
• heart attacks

More than 6000 patients world-wide have received nisoldipine in clinical trials for the treatment of hypertension, either as the immediate release or the Sular extended release formulation.

Of about 1,500 patients who received Sular in hypertension studies, about 55% were exposed for at least 2 months and about one third were exposed for over 6 months, the great majority at doses equivalent to 17 mg and above.

Sular is generally well-tolerated. In the U.S. clinical trials of Sular in hypertension, 10.9% of the 921 Sular patients discontinued treatment due to adverse events compared with 2.9% of 280 placebo patients. The frequency of discontinuations due to adverse experiences was related to dose, with a 5.4% and 10.9% discontinuation rate at the lowest and highest daily dose, respectively.

The most frequently occurring adverse experiences with Sular are those related to its vasodilator properties; these are generally mild and only occasionally lead to patient withdrawal from treatment.

The table below, from U.S. placebo-controlled parallel dose response trials of Sular using doses across the clinical dosage range in patients with hypertension, lists all of the adverse events, regardless of the causal relationship to Sular, for which the overall incidence on Sular was both >1% and greater with Sular than with placebo.

The common adverse events occurred at about the same rate in men as in women, and at a similar rate in patients over age 65 as in those under that age, except that headache was much less common in older patients. Except for peripheral edema and vasodilation, which were more common in whites, adverse event rates were similar in blacks and whites.

The following adverse events occurred in ≤1% of all patients treated for hypertension in U.S. and foreign clinical trials, or with unspecified incidence in other studies. Although a causal relationship of Sular to these events cannot be established, they are listed to alert the physician to a possible relationship with Sular treatment.

Body As A Whole: cellulitis, chills, facial edema, fever, flu syndrome, malaise

Cardiovascular: atrial fibrillation, cerebrovascular accident, congestive heart failure, first degree AV block, hypertension, hypotension, jugular venous distension, migraine, myocardial infarction, postural hypotension, ventricular extrasystoles, supraventricular tachycardia, syncope, systolic ejection murmur, T wave abnormalities on ECG (flattening, inversion, nonspecific changes), venous insufficiency

Digestive: abnormal liver function tests, anorexia, colitis, diarrhea, dry mouth, dyspepsia, dysphagia, flatulence, gastritis, gastrointestinal hemorrhage, gingival hyperplasia, glossitis, hepatomegaly, increased appetite, melena, mouth ulceration

Endocrine: diabetes mellitus, thyroiditis

Hemic and Lymphatic: anemia, ecchymoses, leukopenia, petechiae

Metabolic and Nutritional: gout, hypokalemia, increased serum creatine kinase, increased nonprotein nitrogen, weight gain, weight loss

Musculoskeletal: arthralgia, arthritis, leg cramps, myalgia, myasthenia, myositis, tenosynovitis

Nervous: abnormal dreams, abnormal thinking and confusion, amnesia, anxiety, ataxia, cerebral ischemia, decreased libido, depression, hypesthesia, hypertonia, insomnia, nervousness, paresthesia, somnolence, tremor, vertigo

Respiratory: asthma, dyspnea, end inspiratory wheeze and fine rales, epistaxis, increased cough, laryngitis, pharyngitis, pleural effusion, rhinitis, sinusitis

Skin and Appendages: acne, alopecia, dry skin, exfoliative dermatitis, fungal dermatitis, herpes simplex, herpes zoster, maculopapular rash, pruritus, pustular rash, skin discoloration, skin ulcer, sweating, urticaria

Special Senses: abnormal vision, amblyopia, blepharitis, conjunctivitis, ear pain, glaucoma, itchy eyes, keratoconjunctivitis, otitis media, retinal detachment, tinnitus, watery eyes, taste disturbance, temporary unilateral loss of vision, vitreous floater

Urogenital: dysuria, hematuria, impotence, nocturia, urinary frequency, increased BUN and serum creatinine, vaginal hemorrhage, vaginitis

The following postmarketing event has been reported very rarely in patients receiving Sular:

• systemic hypersensitivity reaction which may include one or more of the following;
• angioedema,
• shortness of breath,
• tachycardia,
• chest tightness,
• hypotension, and
• rash.

A definite causal relationship with Sular has not been established. An unusual event observed with immediate release nisoldipine but not observed with Sular was one case of photosensitivity. Gynecomastia has been associated with the use of calcium channel blockers.

A 30 to 45% increase in AUC and Cmax of nisoldipine was observed with concomitant administration of cimetidine 400 mg twice daily.

Ranitidine 150 mg twice daily did not interact significantly with nisoldipine (AUC was decreased by 15 -20%). No pharmacodynamic effects of either histamine H2 receptor antagonist were observed.