Bisacodyl-K may be available in the countries listed below.
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Betoptic® Sterile Ophthalmic Solution contains betaxolol hydrochloride, a cardioselective beta-adrenergic receptor blocking agent, in a sterile isotonic solution. Betaxolol hydrochloride is a white, crystalline powder, soluble in water, with a molecular weight of 343.89. The chemical structure is presented below:
Empirical Formula:
C18H29NO3•HCl
Chemical Name:
(±) - 1 - [p - [2 - (Cyclopropylmethoxy)ethyl]phenoxy] - 3 - (isopropylamino) - 2 - propanol hydrochloride.
Each mL of Betoptic Ophthalmic Solution (0.5%) contains: Active: 5.6 mg betaxolol hydrochloride equivalent to betaxolol base 5 mg. Preservative: Benzalkonium Chloride 0.01%. Inactive: Edetate Disodium, Sodium Chloride, Hydrochloric Acid and/or Sodium Hydroxide (to adjust pH), and Purified Water. DM-00
Betaxolol HCl, a cardioselective (beta-1-adrenergic) receptor blocking agent, does not have significant membrane-stabilizing (local anesthetic) activity and is devoid of intrinsic sympathomimetic action. Orally administered beta-adrenergic blocking agents reduce cardiac output in healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-adrenergic receptor antagonists may inhibit the sympathetic stimulatory effect necessary to maintain adequate cardiac function.
When instilled in the eye, Betoptic Ophthalmic Solution has the action of reducing elevated as well as normal intraocular pressure, whether or not accompanied by glaucoma. Ophthalmic betaxolol has minimal effect on pulmonary and cardiovascular parameters.
Ophthalmic betaxolol (one drop in each eye) was compared to timolol and placebo in a three-way crossover study challenging nine patients with reactive airway disease who were selected on the basis of having at least a 15% reduction in the forced expiratory volume in one second (FEV1) after administration of ophthalmic timolol. Betaxolol HCl had no significant effect on pulmonary function as measured by FEV1. Forced Vital Capacity (FVC) and FEV1/VC. Additionally, the action of isoproteranol, a beta stimulant, administered at the end of the study was not inhibited by ophthalmic betaxolol. In contrast, ophthalmic timolol significantly decreased these pulmonary functions.
| Means | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Betaxolol 1.0%a | Timolol 0.5% | Placebo | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
1Schoene, R. B. et al., Am. J. Ophthal. 97:86, 1984. aTwice the clinical concentration. bInhaled at 240 minutes; measurement at 270 minutes. *Timolol statistically different from betaxolol and placebo (p < 0.05). | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Baseline | 1.6 | 1.4 | 1.4 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 60 minutes | 2.3 | -25.7* | 5.8 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 120 Minutes | 1.6 | -27.4* | 7.5 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 240 Minutes | -6.4 | -26.9* | 6.9 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Isoproternolb | 36.1 | -12.4* | 42.8 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
No evidence of cardiovascular beta-adrenergic blockade during exercise was observed with betaxolol in a double-masked, three-way crossover study in 24 normal subjects comparing ophthalmic betaxolol, timolol and placebo for effect on blood pressure and heart rate. Mean arterial blood pressure was not affected by any treatment; however, ophthalmic timolol produced a significant decrease in the mean heart rate.
| TREATMENT | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Bruce Stress Exercise Test | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Minutes | Betaxolol 1%a | Timolol 0.5% | Placebo | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
1Atkins, J. M. et. al., Am. J. Oph. 99:173-175, Feb., 1985. aTwice the clinical concentration. *Mean pulse rate significantly lower for timolol than betaxolol or placebo (p < 0.05). | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 0 | 79.2 | 79.3 | 81.2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 2 | 130.2 | 126.0 | 130.4 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 4 | 133.4 | 128.0* | 134.3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 6 | 136.4 | 129.2* | 137.9 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 8 | 139.8 | 131.8* | 139.4 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 10 | 140.8 | 131.8* | 141.3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Optic nerve head damage and visual field loss are the result of a sustained elevated intraocular pressure and poor ocular perfusion. Betoptic Ophthalmic Solution has the action of reducing elevated as well as normal intraocular pressure, and the mechanism of ocular hypotensive action appears to be a reduction of aqueous production as demonstrated by tonography and aqueous fluorophotometry. The onset of action with Betoptic Ophthalmic Solution can generally be noted within 30 minutes and the maximal effect can usually be detected 2 hours after topical administration. A single dose provides a 12-hour reduction in intraocular pressure. Clinical observation of glaucoma patients treated with Betoptic Ophthalmic Solution for up to three years shows that the intraocular pressure lowering effect is well maintained.
Clinical studies show that topical Betoptic Ophthalmic Solution reduces mean intraocular pressure 25% from baseline. In trials using 22 mmHg as a generally accepted index of intraocular pressure control, Betoptic Ophthalmic Solution was effective in more than 94% of the population studied, of which 73% were treated with the beta blocker alone. In controlled, double-masked studies, the magnitude and duration of the ocular hypotensive affect of Betoptic Ophthalmic Solution and ophthalmic timolol solution were clinically equivalent.
Betoptic Ophthalmic Solution has also been used successfully in glaucoma patients who have undergone a laser trabeculoplasty and have needed additional long-term ocular hypotensive therapy.
Betoptic Ophthalmic Solution has been well tolerated in glaucoma patients wearing hard or soft contact lenses and in aphakic patients.
Betoptic Ophthalmic Solution does not produce miosis or accommodative spasm which are frequently seen with miotic agents. The blurred vision and night blindness often associated with standard miotic therapy are not associated with Betoptic Ophthalmic Solution. Thus, patients with central lenticular opacities avoid the visual impairment caused by a constricted pupil.
Betoptic Ophthalmic Solution has been shown to be effective in lowering intraocular pressure and is indicated in the treatment of ocular hypertension and chronic open-angle glaucoma. It may be used alone or in combination with other anti-glaucoma drugs.
In clinical studies Betoptic was safely used to lower intraocular pressure in 47 patients with both glaucoma and reactive airway disease who were followed for a mean period of 15 months. However, caution should be used in treating patients with severe reactive airway disease or a history of asthma.
Hypersensitivity to any component of this product. Betoptic Ophthalmic Solution is contraindicated in patients with sinus bradycardia, greater than a first degree atrioventricular block, cardiogenic shock, or patients with overt cardiac failure.
Topically applied beta-adrenergic blocking agents may be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported with topical application of beta-adrenergic blocking agents.
Betoptic® Ophthalmic Solution has been shown to have a minor effect on heart rate and blood pressure in clinical studies. Caution should be used in treating patients with a history of cardiac failure or heart block. Treatment with Betoptic Ophthalmic Solution should be discontinued at the first signs of cardiac failure.
Information for Patients. Do not touch dropper tip to any surface as this may contaminate the solution.
Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.
Beta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents, which might precipitate a thyroid storm.
Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopla, ptosis, and generalized weakness).
Consideration should be given to the gradual withdrawal of beta-adrenergic blocking agents prior to general anesthesia because of the reduced ability of the heart to respond to beta-adrenergically mediated sympathetic reflex stimuli.
Caution should be exercised in the treatment of glaucoma patients with excessive restriction of pulmonary function. There have been reports of asthmatic attacks and pulmonary distress during betaxolol treatment. Although rechallenges of some such patients with ophthalmic betaxolol has not adversely affected pulmonary function test results, the possibility of adverse pulmonary effects in patients sensitive to beta blockers cannot be ruled out.
While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.
Patients who are receiving a beta-adrenergic blocking agent orally and Betoptic Ophthalmic Solution should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta blockade.
Close observation of the patients is recommended when a beta blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or bradycardia.
Betaxolol is an adrenergic blocking agent; therefore, caution should be exercised in patients using concomitant adrenergic psychotropic drugs.
In patients with angle-closure glaucoma, the immediate treatment objective is to reopen the angle by constriction of the pupil with a miotic agent. Betaxolol has little or no effect on the pupil. When the Betoptic Ophthalmic Solution is used to reduce elevated intraocular pressure in angle-closure glaucoma, it should be used with a miotic and not alone.
Lifetime studies with betaxolol HCl have been completed in mice at oral doses of 6, 20 or 60 mg/kg/day and in rats at 3, 12, or 48 mg/kg/day; betaxolol HCl demonstrated no carcinogenic effect. Higher dose levels were not tested.
In a variety of in vitro and in vivo bacterial and mammalian cell assays, betaxolol HCl was nonmutagenic.
Pregnancy Category C. Reproduction, teratology, and peri- and postnatal studies have been conducted with orally administered betaxolol HCl in rats and rabbits. There was evidence of drug related postimplantation loss in rabbits and rats at dose levels above 12 mg/kg and 128 mg/kg, respectively. Betaxolol HCl was not shown to be teratogenic, however, and there were no other adverse effects on reproduction at subtoxic dose levels. There are no adequate and well-controlled studies in pregnant women. Betoptic Ophthalmic Solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether betaxolol HCl is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when BEOPTIC Ophthalmic Solution is administered to nursing women.
Safety and effectiveness in pediatric patients have not been established.
The following adverse reactions have been reported in clinical trials with Betoptic Ophthalmic Solution.
Discomfort of short duration was experienced by one in four patients, but none discontinued therapy; occasional tearing has been reported. Rare instances of decreased corneal sensitivity, erythema, itching sensation, corneal punctate staining, keratitis, anisocoria, edema, and photophobia have been reported.
Additional medical events reported with other formulations of betaxolol include blurred vision, foreign body sensation, dryness of the eyes, inflammation, discharge, ocular pain, decreased visual acuity, and crusty lashes.
Systemic reactions following administration of Betoptic Ophthalmic Solution 0.5% or Betoptic S Ophthalmic Suspension 0.25% have been rarely reported. These include:
Bradycardia, heart block and congestive failure.
Pulmonary distress characterized by dyspnea, bronchospasm, thickened bronchial secretions, asthma and respiratory failure.
Insomnia, dizziness, vertigo, headaches, depression, lethargy, and increase in signs and symptoms of myasthenia gravis.
Hives, toxic epidermal necrolysis, hair loss and glossitis.
No information is available on overdosage of humans. The oral LD50 of the drug ranged from 350-920 mg/kg in mice and 860-1050 mg/kg in rats. The symptoms which might be expected with an overdose of a systemically administered beta-1-adrenergic receptor blocker agent are bradycardia, hypotension and acute cardiac failure. A topical overdose of Betoptic Ophthalmic Solution may be flushed from the eye(s) with warm tap water.
The recommended dose is one to two drops of Betoptic Ophthalmic Solution in the affected eye(s) twice daily. In some patients, the intraocular pressure lowering responses to Betoptic Ophthalmic Solution may require a few weeks to stabilize. As with any new medication, careful monitoring of patients is advised.
If the intraocular pressure of the patient is not adequately controlled on this regimen, concomitant therapy with pilocarpine and other miotics, and/or epinephrine and/or carbonic anhydrase inhibitors can be instituted.
Betoptic Ophthalmic Solution is a sterile, isotonic, aqueous solution of betaxolol hydrochloride. Supplied as follows: 2.5, 5, 10 and 15 mL in plastic ophthalmic DROP-TAINER® dispensers.
2.5 mL: NDC 0065-0245-20 10 mL: NDC 0065-0245-10
5 mL: NDC 0065-0245-05 15 mL: NDC 0065-0245-15
Store at room temperature
Rx Only
U.S. Patents Nos. 4,252,984; 4,311,708; 4,342,783
ALCON®
OPHTHALMIC
ALCON LABORATORIES, INC
Fort Worth, Texas 76134 USA
Printed in USA
236015-0598
| Betoptic betaxolol hydrochloride solution/ drops | ||||||||||||||||||||||||
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des-IP-ra-meen
Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term studies with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24, and there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. This risk must be balanced with the clinical need. Monitor patients closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Not approved for use in pediatric patients .
In the U.S.
Available Dosage Forms:
Therapeutic Class: Antidepressant
Pharmacologic Class: Antidepressant, Tricyclic
Desipramine is used to treat mental depression. desipramine is a tricyclic antidepressant (TCA) .
desipramine is available only with your doctor's prescription .
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For desipramine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to desipramine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Appropriate studies have not been performed on the relationship of age to the effects of desipramine in the pediatric population. Safety and efficacy have not been established .
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of desipramine in the elderly. However, confusion and falling are more likely to occur in the elderly, who are usually more sensitive than younger adults to the effects of desipramine. Also, elderly patients may require an adjustment of dosage because of age-related kidney problems .
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking desipramine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using desipramine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
Using desipramine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Using desipramine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
The presence of other medical problems may affect the use of desipramine. Make sure you tell your doctor if you have any other medical problems, especially:
Take desipramine only as directed by your doctor to benefit your condition as much as possible. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered .
desipramine should come with a medication guide. Read and follow these instructions carefully. Ask your doctor if you have any questions .
The dose of desipramine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of desipramine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of desipramine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Do not keep outdated medicine or medicine no longer needed.
It is very important that your doctor check your progress at regular visits to allow for changes in your dose. Blood tests will be needed to check for any unwanted effects .
Desipramine may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed. If you, your child, or your caregiver notice any of these side effects, tell your doctor or your child's doctor right away .
Do not take desipramine if you have taken a monoamine oxidase (MAO) inhibitor (isocarboxazid [e.g., Marplan], phenelzine [e.g., Nardil], selegiline [e.g., Eldepryl], or tranylcypromine [e.g., Parnate]) in the past 2 weeks. Do not start taking a MAO inhibitor within 2 weeks of stopping desipramine. If you do, you may develop confusion, agitation, restlessness, stomach or intestinal symptoms, sudden high body temperature, extremely high blood pressure, or severe convulsions .
Do not stop taking desipramine without first checking with your doctor. Your doctor may want you to reduce gradually the amount you are using before stopping completely. This may help prevent a possible worsening of your condition and reduce the possibility of withdrawal symptoms such as headache, nausea, or a general feeling of discomfort or illness .
desipramine will add to the effects of alcohol and other central nervous system (CNS) depressants (medicines that cause drowsiness). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies or colds; sedatives, tranquilizers, or sleeping medicines; prescription pain medicine or narcotics; barbiturates; medicine for seizures; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are using desipramine.
Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements .
desipramine may raise or lower your blood sugar. If you notice a change in the results of your blood or urine sugar tests or if you have any questions, check with your doctor .
Make sure any doctor or dentist who treats you knows that you are using desipramine. You may need to stop using desipramine several days before having surgery or medical tests .
desipramine may cause some people to become drowsy or less alert than they are normally. Make sure you know how you react to desipramine before you drive, use machines, or do anything else that could be dangerous if you are drowsy or not alert.
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor or nurse immediately if any of the following side effects occur:
Get emergency help immediately if any of the following symptoms of overdose occur:
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
See also: desipramine side effects (in more detail)
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