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BROWSE topics
Urologic Agents
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Urology - Bladder spasm |
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Belladonna and opium - B&O Supprettes ®
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| Drug Category: Analgesic Combination. Urinary Antispasmodic Agent.
Use: Relief of moderate to severe pain associated with rectal or bladder tenesmus that may occur in postoperative states and neoplastic situations. Pain associated with ureteral spasms not responsive to non-narcotic analgesics and to space intervals between injections of opiates. Dosing (Adults): 1 suppository rectally once or twice daily. Max 4 doses/day. Supplied: #15 A: Belladonna extract 16.2 mg and opium 30 mg. #16 A: Belladonna extract 16.2 mg and opium 60 mg. |
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flavoxate (Urispas ®)
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CLINICAL PHARMACOLOGY Flavoxate hydrochloride counteracts smooth muscle spasm of the urinary tract and exerts its effect directly on the muscle. In a single study of 11 normal male subjects, the time to onset of action was 55 minutes. The peak effect was observed at 112 minutes. 57% of the flavoxate HCl was excreted in the urine within 24 hours. INDICATIONS AND USAGE Flavoxate HCl tablets are indicated for symptomatic relief of dysuria, urgency, nocturia, suprapubic pain, frequency and incontinence as may occur in cystitis, prostatitis, urethritis, urethrocystitis/urethrotrigonitis. Flavoxate HCl tablets are not indicated for definitive treatment, but are compatible with drugs used for the treatment of urinary tract infections. CONTRAINDICATIONS Flavoxate HCl tablets are contraindicated in patients who have any of the following obstructive conditions: pyloric or duodenal obstruction, obstructive intestinal lesions or ileus, achalasia, gastrointestinal hemorrhage and obstructive uropathies of the lower urinary tract. WARNINGS Flavoxate HCl should be given cautiously in patients with suspected glaucoma Dosage Children >12 years and Adults: Oral: 100-200 mg 3-4 times/day; reduce the dose when symptoms improve Dietary Considerations Should be taken with water on an empty stomach. Supplied Tablet [film coated], as hydrochloride: 100 mg |
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hyoscyamine (Levsin ®)
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CLINICAL PHARMACOLOGY Levsin® inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of the smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, and the exocrine glands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Levsin® inhibits gastrointestinal propulsive motility and decreases gastric acid secretion. Levsin® also controls excessive pharyngeal, tracheal and bronchial secretions. Levsin® is absorbed totally and completely by sublingual administration as well as oral administration. Once absorbed, Levsin® disappears rapidly from the blood and is distributed throughout the entire body. The half-life of Levsin® is 2 to 3½ hours. Levsin® is partly hydrolyzed to tropic acid and tropine but the majority of the drug is excreted in the urine unchanged within the first 12 hours. Only traces of this drug are found in breast milk. Levsin® passes the blood brain barrier and the placental barrier. Dosage Children >12 years and Adults: Gastrointestinal disorders: 0.125-0.25 mg every 4 hours or as needed (before meals or food); maximum: 1.5 mg/24 hours. Cystospaz®: 0.15-0.3 mg up to 4 times/day. Oral (timed release): Children >12 years and Adults: Gastrointestinal disorders: 0.375-0.75 mg every 12 hours; maximum: 1.5 mg/24 hours I.M., I.V., SubQ: Children >12 years and Adults: Gastrointestinal disorders: 0.25-0.5 mg; may repeat as needed up to 4 times/day, at 4-hour intervals I.V.: Adults: Diagnostic procedures: 0.25-0.5 mg given 5-10 minutes prior to procedure To reduce drug-induced bradycardia during surgery: 0.125 mg; repeat as needed To reverse neuromuscular blockade: 0.2 mg for every 1 mg neostigmine (or the physostigmine/pyridostigmine equivalent) Supplied Capsule, timed release, as sulfate (Cystospaz-M® [DSC], Levsinex®): 0.375 mg Elixir, as sulfate: 0.125 mg/5 mL (480 mL) Hyosine: 0.125 mg/5 mL (480 mL) Levsin®: 0.125 mg/5 mL (480 mL) [contains alcohol 20%; orange flavor] Injection, solution, as sulfate (Levsin®): 0.5 mg/mL (1 mL) Solution, oral drops, as sulfate: 0.125 mg/mL (15 mL) Hyosine: 0.125 mg/mL (15 mL) Levsin®: 0.125 mg/mL (15 mL) [contains alcohol 5%; orange flavor] Tablet (Cystospaz®): 0.15 mg Tablet, orally-disintegrating, as sulfate (NuLev™): 0.125 mg [contains phenylalanine 1.7 mg/tablet, mint flavor] Tablet, sublingual, as sulfate: 0.125 mg Levsin/SL®: 0.125 mg [peppermint flavor] Symax SL: 0.125 mg |
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Bladder instability (Overactive bladder) |
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darifenacin (Enablex ® )
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CLINICAL PHARMACOLOGY
General Darifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9- and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs INDICATIONS AND USAGE ENABLEX® (darifenacin) extended-release tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency. CONTRAINDICATIONS ENABLEX® (darifenacin) extended-release tablets are contraindicated in patients with urinary retention, gastric retention or uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. ENABLEX is also contraindicated in patients with known hypersensitivity to the drug or its ingredients. Dosing (Adults): Symptoms of bladder overactivity - Initial: 7.5 mg orally once daily. If response is not adequate after a minimum of 2 weeks, dosage may be increased to 15 mg once daily. Dosage should not be increased in patients with hepatic impairment or in those receiving potent inhibitors of CYP3A4. Hepatic dosing: Moderate impairment (Child-Pugh Class B): Daily dosage should not exceed 7.5 mg/day. Severe impairment (Child-Pugh Class C): Use is not recommended. Supplied: Extended release tablet: 7.5 mg, 15 mg. |
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oxybutynin (Ditropan ®)
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CLINICAL PHARMACOLOGY Oxybutynin chloride exerts a direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. Oxybutynin chloride exhibits only one fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects). Oxybutynin chloride relaxes bladder smooth muscle. In patients with conditions characterized by involuntary bladder contractions, cystometric studies have demonstrated that oxybutynin chloride increases bladder (vesical) capacity, diminishes the frequency of uninhibited contractions of the detrusor muscle, and delays the initial desire to void. Oxybutynin chloride thus decreases urgency and the frequency of both incontinent episodes and voluntary urination. Antimuscarinic activity resides predominately in the R-isomer. A metabolite, desethyloxybutynin, has pharmacological activity similar to that of oxybutynin in in vitro studies. Exhibits 20% of the anticholinergic activity of atropine, however, has 4 to 10 times the antispasmodic activity. INDICATIONS AND USAGE DITROPAN® (oxybutynin chloride) is indicated for the relief of symptoms of bladder instability associated with voiding in patients with uninhibited neurogenic or reflex neurogenic bladder (i.e., urgency, frequency, urinary leakage, urge incontinence, dysuria). CONTRAINDICATIONS DITROPAN® (oxybutynin chloride) is contraindicated in patients with urinary retention, gastric retention and other severe decreased gastrointestinal motility conditions, uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. DITROPAN is also contraindicated in patients who have demonstrated hypersensitivity to the drug substance or other components of the product. Dosing (Adults): Oral: 5 mg 2-3 times/day up to 5 mg 4 times/day maximum. Extended release: Initial: 5-10 mg once daily, may increase in 5-10 mg increments; maximum: 30 mg daily. Transdermal: Adults: Apply one 3.9 mg/day patch twice weekly (every 3-4 days). Note: Should be discontinued periodically to determine whether the patient can manage without the drug and to minimize resistance to the drug Elderly: 2.5 to 5 mg 2-3 times/day Administration Oral: Immediate release tablets and solution should be administered on an empty stomach with water. Extended release tablets may be taken with or without food and must be swallowed whole; do not crush, divide, or chew. Transdermal: Apply to clean, dry skin on abdomen, hip, or buttock. Select a new site for each new system (avoid re-application to same site within 7 days). Supplied Syrup, as chloride (Ditropan®): 5 mg/5 mL (473 mL) Tablet, as chloride (Ditropan®): 5 mg Tablet, extended release, as chloride (Ditropan® XL): 5 mg, 10 mg, 15 mg Transdermal system (Oxytrol™): 3.9 mg/day (8s, 24s) [39 cm 2 ; total oxybutynin 36 mg] |
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solifenacin (Vesicare ® )
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Clinical Pharmacology Solifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion. INDICATIONS AND USAGE VESIcare is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. CONTRAINDICATIONS VESIcare is contraindicated in patients with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, and in patients who have demonstrated hypersensitivity to the drug substance or other components of the product. Dosing (Adults): Overactive bladder: 5 mg orally once daily. If tolerated, may increase to 10 mg orally once daily. Renal Dosing: Use with caution in patients with reduced renal function ( Clcr <30 ml/minute: 5 mg/day). Hepatic impairment: Use with caution in reduced hepatic function: Moderate: 5 mg/day. Severe impairment: Not recommended. Supplied: 5 mg, 10 mg tablet. |
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tolterodine (Detrol ® )
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CLINICAL PHARMACOLOGY Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. Effects on urodynamic parameters before and 1 and 5 hours after a single 6.4 mg dose of tolterodine immediate release were determined in healthy volunteers. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract. INDICATIONS AND USAGE DETROL Tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. CONTRAINDICATIONS DETROL Tablets are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. DETROL is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients. Dosing (Adults): Immediate release tablet: 2 mg orally twice daily. The dose may be lowered to 1 mg twice daily based on individual response and tolerability. Extended release capsule: 4 mg once a day- dose may be lowered to 2 mg daily based on individual response and tolerability. Renal Dosing (Crcl 10-30)/ hepatic impairment: Use with caution. 1 mg twice daily (regular release) or 2 mg daily (extended release). Supplied: 1 mg, 2 mg tablet. 2 mg, 4mg extended release capsule. |
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trospium (Sanctura ® )
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| CLINICAL PHARMACOLOGY SANCTURA® is an antispasmodic, antimuscarinic agent. Trospium chloride antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder. Receptor assays showed that trospium chloride has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses. INDICATIONS AND USAGE SANCTURA® is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. CONTRAINDICATIONS SANCTURA® is contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. SANCTURA® is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients. Dosing (Adults): Overactive bladder - 20 mg orally twice daily. In patients >75 years old or if crcl < 30 ml/min decrease dose to 20 mg once daily at bedtime. Supplied: 20 mg tablet. |
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any diagnosis or treatment made in reliance thereon. David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc. |
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