Ralsin

Ralsin (Ralsin), an α₁-selective adrenoceptor-blocking agent, is a quinazoline derivative. It is piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetra-hydro-2-furanyl)carbonyl]-, monohydrochloride, dihydrate.

Ralsin is a white, crystalline substance, freely soluble in water and isotonic saline and has a molecular weight of 459.93.

Inactive Ingredients: Corn starch, lactose, magnesium stearate, povidone and talc. In addition, 2-mg tab contains FD & C Yellow No. 6 and the 5-mg tab contains iron oxide.

Ralsin (Ralsin hydrochloride) is indicated for the treatment of symptomatic benign prostatic hyperplasia (BPH). There is a rapid response, with approximately 70% of patients experiencing an increase in urinary flow and improvement in symptoms of BPH when treated with Ralsin (Ralsin). The long-term effects of Ralsin (Ralsin) on the incidence of surgery, acute urinary obstruction or other complications of BPH are yet to be determined.

Ralsin (Ralsin) tablets are also indicated for the treatment of hypertension. Ralsin (Ralsin) tablets can be used alone or in combination with other antihypertensive agents such as diuretics or beta-adrenergic blocking agents.

Ralsin is used to treat high blood pressure (hypertension).

High blood pressure adds to the work load of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled.

Ralsin helps to lower blood pressure by relaxing blood vessels so that blood passes through them more easily.

Ralsin is also used to treat benign enlargement of the prostate (benign prostatic hyperplasia [BPH]). Benign enlargement of the prostate is a problem that can occur in men as they get older. The prostate gland is located below the bladder. As the prostate gland enlarges, certain muscles in the gland may become tight and get in the way of the tube that drains urine from the bladder. This can cause problems in urinating, such as a need to urinate often, a weak stream when urinating, or a feeling of not being able to empty the bladder completely.

Ralsin helps relax the muscles in the prostate and the opening of the bladder. This may help increase the flow of urine and/or decrease the symptoms. However, Ralsin will not help shrink the prostate. The prostate may continue to grow. This may cause the symptoms to become worse over time. Therefore, even though Ralsin may lessen the problems caused by enlarged prostate now, surgery still may be needed in the future.

Ralsin is available only with your doctor's prescription.

If Ralsin (Ralsin) administration is discontinued for several days, therapy should be reinstituted using the initial dosing regimen.

Benign Prostatic Hyperplasia

Initial Dose

1 mg at bedtime is the starting dose for all patients, and this dose should not be exceeded as an initial dose. Patients should be closely followed during initial administration in order to minimize the risk of severe hypotensive response.

Subsequent Doses

The dose should be increased in a stepwise fashion to 2 mg, 5 mg, or 10 mg once daily to achieve the desired improvement of symptoms and/or flow rates. Doses of 10 mg once daily are generally required for the clinical response. Therefore, treatment with 10 mg for a minimum of 4–6 weeks may be required to assess whether a beneficial response has been achieved. Some patients may not achieve a clinical response despite appropriate titration. Although some additional patients responded at a 20 mg daily dose, there was an insufficient number of patients studied to draw definitive conclusions about this dose. There are insufficient data to support the use of higher doses for those patients who show inadequate or no response to 20 mg daily.

Use with Other Drugs

Caution should be observed when Ralsin (Ralsin) tablets are administered concomitantly with other antihypertensive agents, especially the calcium channel blocker verapamil, to avoid the possibility of developing significant hypotension. When using Ralsin (Ralsin) tablets and other antihypertensive agents concomitantly, dosage reduction and retitration of either agent may be necessary. Concomitant administration of Ralsin (Ralsin) with a PDE-5 inhibitor can result in additive blood pressure lowering effects and symptomatic hypotension; therefore PDE-5 inhibitor therapy should be initiated at the lowest dose in patients taking Ralsin (Ralsin).

Hypertension

The dose of Ralsin (Ralsin) and the dose interval (12 or 24 hours) should be adjusted according to the patient's individual blood pressure response. The following is a guide to its administration:

Initial Dose

1 mg at bedtime is the starting dose for all patients, and this dose should not be exceeded. This initial dosing regimen should be strictly observed to minimize the potential for severe hypotensive effects.

Subsequent Doses

The dose may be slowly increased to achieve the desired blood pressure response. The usual recommended dose range is 1 mg to 5 mg administered once a day; however, some patients may benefit from doses as high as 20 mg per day. Doses over 20 mg do not appear to provide further blood pressure effect and doses over 40 mg have not been studied. Blood pressure should be monitored at the end of the dosing interval to be sure control is maintained throughout the interval. It may also be helpful to measure blood pressure 2-3 hours after dosing to see if the maximum and minimum responses are similar, and to evaluate symptoms such as dizziness or palpitations which can result from excessive hypotensive response. If response is substantially diminished at 24 hours an increased dose or use of a twice daily regimen can be considered. If Ralsin administration is discontinued for several days or longer, therapy should be reinstituted using the initial dosing regimen. In clinical trials, except for the initial dose, the dose was given in the morning.

Use With Other Drugs

How supplied

Ralsin tablets (Ralsin hydrochloride tablets) are available in four dosage strengths:

1 mg, white tablets (bears the Abbott “A” logo and the Abbo-Code DF): Bottles of 100 (NDC 0074-3322-13).

2 mg, orange tablets (bears the Abbott “A” logo and the Abbo-Code DH): Bottles of 100 (NDC 0074-3323-13).

5 mg, tan tablets (bears the Abbott “A” logo and the Abbo-Code DJ): Bottles of 100 (NDC 0074-3324-13).

10 mg, green tablets (bears the Abbott “A” logo and the Abbo-Code DI): Bottles of 100 (NDC 0074-3325-13).

Recommended storage

Store below 86°F (30°C).

Abbott Laboratories. North Chicago, IL 60064, U.S.A.

See also:
What is the most important information I should know about Ralsin?

You should not use this medication if you are allergic to Ralsin.

Ralsin may cause dizziness or fainting, especially when you first start taking it or when you start taking it again. You may wish to take this medication only at bedtime if it causes you to feel light-headed. Be careful if you drive or do anything that requires you to be alert. Avoid standing for long periods of time or becoming overheated during exercise and in hot weather. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

If you stop taking Ralsin for any reason, call your doctor before you start taking it again. You may need a dose adjustment.

Ralsin can affect your pupils during cataract surgery. Tell your eye surgeon ahead of time that you are using this medication. Do not stop using Ralsin before surgery unless your surgeon tells you to.

Tell your doctor about all other medications you use, especially other blood pressure medications including diuretics (water pills).

Use Ralsin as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Ralsin by mouth with or without food.
• Ralsin may cause a sudden drop in blood pressure after the first dose. Take your first dose at bedtime. If you get up during the night, sit up slowly, then stand slowly.
• If you miss a dose of Ralsin, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once. If more than one dose is missed, contact your doctor or pharmacist.

Ask your health care provider any questions you may have about how to use Ralsin.

Use: Labeled Indications

Benign prostatic hyperplasia: Treatment of symptomatic benign prostatic hyperplasia (BPH)

Hypertension: Management of hypertension. Note: Alpha blockers are not recommended as first line therapy (ACC/AHA [Whelton 2017]).

Off Label Uses

Ureteral calculi expulsion

Use of alpha-1 adrenergic blockers, including Ralsin, for treating ureteral calculi is supported by data from a meta-analysis as well as numerous controlled trials. Tamsulosin has the most data, but Ralsin has also demonstrated efficacy in facilitating expulsion of ureteral stones (<10 mm) as medical therapy alone or as an adjunct to shock wave lithotripsy and uteroscopy. Some trials indicate a class effect of alpha-1 adrenergic blockers, with Ralsin reported to be equally effective as tamsulosin, doxazosin, and alfuzosin.

See also:
What other drugs will affect Ralsin?

Concomitant administration of Ralsin (Ralsin) with a phosphodiesterase-5 (PDE-5) inhibitor can result in additive blood pressure lowering effects and symptomatic hypotension.

In controlled trials, Ralsin (Ralsin) tablets have been added to diuretics, and several beta-adrenergic blockers; no unexpected interactions were observed. Ralsin (Ralsin) tablets have also been used in patients on a variety of concomitant therapies; while these were not formal interaction studies, no interactions were observed. Ralsin (Ralsin) tablets have been used concomitantly in at least 50 patients on the following drugs or drug classes: 1) analgesic/anti-inflammatory (e.g., acetaminophen, aspirin, codeine, ibuprofen, indomethacin); 2) antibiotics (e.g., erythromycin, trimethoprim and sulfamethoxazole); 3) anticholinergic/sympathomimetics (e.g., phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseudoephedrine hydrochloride); 4) antigout (e.g., allopurinol); 5) antihistamines (e.g., chlorpheniramine); 6) cardiovascular agents (e.g., atenolol, hydrochlorothiazide, methyclothiazide, propranolol); 7) corticosteroids; 8) gastrointestinal agents (e.g., antacids); 9) hypoglycemics; 10) sedatives and tranquilizers (e.g., diazepam).

Use with Other Drugs

In a study (n=24) where Ralsin and verapamil were administered concomitantly, Ralsin's mean AUC increased 11% after the first verapamil dose and after 3 weeks of verapamil treatment it increased by 24% with associated increases in Cmax (25%) and Cmin (32%) means. Ralsin mean Tmax decreased from 1.3 hours to 0.8 hours after 3 weeks of verapamil treatment. Statistically significant differences were not found in the verapamil level with and without Ralsin. In a study (n=6) where Ralsin and captopril were administered concomitantly, plasma disposition of captopril was not influenced by concomitant administration of Ralsin and Ralsin maximum plasma concentrations increased linearly with dose at steady-state after administration of Ralsin plus captopril.

See also:
What are the possible side effects of Ralsin?

Benign Prostatic Hyperplasia: The incidence of treatment-emergent adverse events has been ascertained from clinical trials conducted worldwide. All adverse events reported during these trials were recorded as adverse reactions. The incidence rates presented as follows are based on combined data from 6 placebo-controlled trials involving once-a-day administration of Ralsin at doses ranging from 1-20 mg. Table 3 summarizes those adverse events reported for patients in these trials when the incidence rate in the Ralsin group was at least 1% and was greater than that for the placebo group, or where the reaction is of clinical interest. Asthenia, postural hypotension, dizziness, somnolence, nasal congestion/rhinitis and impotence were the only events that were significantly more common (p≤0.05) in patients receiving Ralsin than in patients receiving placebo. The incidence of urinary tract infection was significantly lower in the patients receiving Ralsin than in patients receiving placebo. An analysis of the incidence rate of hypotensive adverse events adjusted for the length of drug treatment has shown that the risk of the events is greatest during the initial 7 days of treatment, but continues at all time intervals. See Table 3.

Additional adverse events have been reported but these are, in general, not distinguishable from symptoms that might have occurred in the absence of exposure to Ralsin. The safety profile of patients treated in the long-term open-label study was similar to that observed in the controlled studies.

The adverse events were usually transient and mild or moderate in intensity, but sometimes were serious enough to interrupt treatment. In the placebo-controlled clinical trials, the rates of premature termination due to adverse events were not statistically different between the placebo and Ralsin groups. The adverse events that were bothersome, as judged by their being reported as reasons for discontinuation of therapy by at least 0.5% of the Ralsin group and being reported more often than in the placebo group, are shown in Table 4.

Hypertension: The prevalence of adverse reactions has been ascertained from clinical trials conducted primarily in the United States. All adverse experiences (events) reported during these trials were recorded as adverse reactions. The prevalence rates presented as follows are based on combined data from 14 placebo-controlled trials involving once-a-day administration of Ralsin, as monotherapy or in combination with other antihypertensive agents, at doses ranging from 1-40 mg. Table 5 summarizes those adverse experiences reported for patients in these trials where the prevalence rate in the Ralsin group was at least 5%, where the prevalence rate for the Ralsin group was at least 2% and was greater than the prevalence rate for the placebo group, or where the reaction is of particular interest. Asthenia, blurred vision, dizziness, nasal congestion, nausea, peripheral edema, palpitations and somnolence were the only symptoms that were significantly more common (p<0.05) in patients receiving Ralsin than in patients receiving placebo. Similar adverse reaction rates were observed in placebo-controlled monotherapy trials. See Table 5.

Additional adverse reactions have been reported, but these are, in general, not distinguishable from symptoms that might have occurred in the absence of exposure to Ralsin. The following additional adverse reactions were reported by at least 1% of 1987 patients who received Ralsin in controlled or open, short- or long-term clinical trials or have been reported during marketing experience:

Body as a Whole: Chest pain, facial edema, fever, abdominal pain, neck pain, shoulder pain.

Cardiovascular System: Arrythmia, vasodilation.

Digestive System: Constipation, diarrhea, dry mouth, dyspepsia, flatulence, vomiting.

Metabolic/Nutritional Disorders: Gout.

Muscoloskeletal System: Arthralgia, arthritis, joint disorder, myalgia.

Nervous System: Anxiety, insomnia.

Respiratory System: Bronchitis, cold symptoms, epistaxis, flu symptoms, increased cough, pharyngitis, rhinitis.

Skin and Appendages: Pruritus, rash, sweating.

Special Senses: Abnormal vision, conjunctivitis, tinnitus.

Urogenital System: Urinary frequency, urinary incontinence primarily reported in postmenopausal women, urinary tract infection.

Post-marketing experience indicates that in rare instances, patients may develop allergic reactions, including anaphylaxis, following administration of Ralsin tablets.

The adverse reactions were usually mild or moderate in intensity but sometimes were serious enough to interrupt treatment. The adverse reactions that were most bothersome, as judged by their being reported as reasons for discontinuation of therapy by at least 0.5% of the Ralsin group and being reported more often than in the placebo group, are shown in Table 6.