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Archive for the ‘Antipsychotic Agents’


12/05, 2007

Benzisoxazole-Derivatives - Guidelines for Using

Type of Drug:

Atypical antipsychotic.

How the Drug Works:

The exact mechanism of action, like other drugs used to treat schizophrenia, is not known. Benzisoxazole drugs may work by antagonizing dopamine type 2 and Sheraton type 2 receptors in the brain.

Uses:

For treatment of schizophrenia.

Precautions:

Tardive dyskinesia: Involuntary and uncontrollable movements may develop in patients treated with antipsychotic drugs. Occurrence is highest in the elderly, especially women. However, it is impossible to predict which patients are likely to develop the syndrome. The risk of developing these involuntary movements and the likelihood they will become permanent are increased with long-term use and with high doses. However, it is possible to develop these symptoms after short­term treatment at low doses. The syndrome is characterized by rhythmical, involuntary movements of tongue, face, mouth, or jaw (eg, protrusion of tongue, puffing of cheeks, puckering of mouth, chewing movements), sometimes accompanied by involuntary movements of the arms and legs. Fine worm-like movement of the tongue may be an early sign of the

syndrome . If the medication is stopped at this time, the may not develop further. There is no known treatment for established case of tardive dyskinesia, although the syndrome may stop, partially or cell politely, if the drug is withdrawn. Antipsychotic treatment, however, my suppress or partially suppress the signs and symptoms of the syndrome and thereby may possibly mask the underlying disease process; The effect that symptomatic suppression has upon the long-term scour of the syndrome is unknown.

Neuroleptic Malignant Syndrome (NMS) Is a potentially fatal syndrome associated with antipsychotic drugs. Symptoms include fever, muscle rigidity, altered mental abilities, irregular pulse and blood pressure, Increased heart rate, sweating, and irregular heart rhythm.

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Use only if clearly needed and potential benefits weigh the possible hazards to the fetus.

Breastfeeding: It is not known if benisoxazole derivatives appear in brest milk. It is recommended that women not breastfeed while receiving these drug.

Children: The safety and effectiveness in patients younger than 18 years of age have not been established.

Elderly: Dose modifications (eg, lower starting dose) of dispersion may be necessary. Ziprasidone injection has not been evaluated in patients 65 years of age and older.

Lab Tests: Lab tests may be required to monitor ziprasidone therapy. Tests include serum potassium and magnesium levels.

Drug Interactions:

Tell your doctor or pharmacist if you are taking or planning to take any over­the-counter or prescription medications or dietary supplements with these drugs. Doses of one or both drugs may need to be modified or a different drug may need to be prescribed. The following drugs and drug classes interact with these drugs:

  • Antihypertensive agents (eg, hydrochlorothiazide)
  • Carbamazepine (eg, Tegretol)
  • Centrally acting drugs (eg, guanfacine, tramadol)
  • Clozapine (eg, Clozaril)
  • Dopamine agonists (eg, pramipexole)
  • Drugs that prolong the OT interval (eg, chlorpromazine, quinidine, sparfloxacin)
  • Fluoxetine (eg, Prozac)
  • Ketoconazole (eg, Nizoral)

Side Effects:

Every drug is capable of producing side effects. Many patients experience no, or minor, side effects. The frequency and severity of side effects depend on many factors including dose, duration of therapy, and individual susceptibility. Possible side effects include:

Digestive Tract: Nausea; constipation; indigestion; diarrhea; dry mouth; vomiting; stomach pain; increased or decreased saliva; toothache; appetite loss.

Respiratory System: Upper respiratory infection; cough; rhinitis; sinus infection; sore throat; difficulty breathing; runny nose.

Nervous System: Sleepiness; dizziness; inability to sit still; muscle tension; headache; anxiety; agitation; increased dream activity; abnormal tongue, face, jaw, or mouth movements; involuntary arm and leg movements; tremor; shuffling; rigidity.

Circulatory System: Increased or decreased heart rate; postural hypotension (light-headedness when rising quickly from sitting or lying position); increased blood pressure.

Skin: Rash; skin irritation; dry skin; sensitivity to light.

Other: Weakness; muscle pain; joint pain; fainting; dizziness; erectile dysfunction; weight gain; decreased sexual desire; abnormal vision.

Guidelines for Use:

  • Dosage is individualized. Take exactly as prescribed.
  • Do not stop taking or change the dose unless instructed by your doctor.
  • Swallow the ziprasidone capsules whole; take with food.
  • It is best to take ziprasidone at the same time each day.
  • It may take a few weeks for this medicine to start working. Continue taking the medication, even when you feel better.
  • Avoid alcohol while taking this medicine.
  • Use caution in hot weather; be careful not to become dehydrated.
  • Notify your doctor immediately if you experience fever, perspiration, muscle rigidity, involuntary movements, abnormal heart rate or rhythm, or fainting.
  • May cause drowsiness. Use caution while driving or performing other tasks requiring alertness, coordination, or physical dexterity.
  • This medicine may cause dizziness, light-headedness, or fainting, especially when rising or standing. If these symptoms occur, sit or lie down. Contact your doctor if they continue.
  • Inform your doctor if you are pregnant, become pregnant, are planning to become pregnant, or if you are breastfeeding.
  • Lab tests may be required to monitor therapy. Be sure to keep appointments.
  • Store at controlled room temperature (59° to 86°F). Protect from light and moisture.

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11/20, 2007

How Phenylbutylpiperadine Derivatives Works?

Type of Drug:

Typical (conventional) antipsychotics.

How the Drug Works:

The mechanism of action is not well defined, but thought to be related to central dopamine receptor antagonist activity.

Uses:

Haloperidol is used in the management of manifestations of serious psychotic disorders, including schizophrenia.

Pimozide and haloperidol may be used to suppress motor and phonic tics in patients with Turreted disorder who have failed to respond to standard treatment.

Unlabeled Uses: Bipolar disorder; management of patients with demetiarelated psychotic symptoms.

Tardive dyskinesia: Involuntary and uncontrollable movements may develop in patients treated with antipsychotic drugs. Occurrence is highest in the elderly, especially women. However, it is impossible to predict which patients are likely to develop the syndrome. The risk of developing these involuntary movements and the likelihood they will become permanent are increased with long-term use and with high doses. However, it is possible to develop these symptoms after short­term treatment at low doses. The syndrome is character rhythmcal, involuntary movements of tongue, face, mouth, of jaw (eg,protrusion of tongue, puffing of Cheeks, plucking of mouth chewing movement sometimes accompanied by involuntary movements of the arms and ages. Fine worm-like movement of the tongue may be an early sign of the syndrome. If the medication is stopped at this time, the syndrome may not develop further. There is no known treatment for established cases of tardive dyskinesia, although the syndrome may stop, partially or completely, if the drug is withdrawn. Anti psychotic treatment, however, may suppress or partially suppress the signs and symptoms of the syndrome and thereby may possibly mask the underlying disease process. The effect that symptomatic suppression has upon the long-term course of the syndrome is unknown.

Neuroleptic Malignant Syndrome (NMS) Is a potentially fatal syndrome associated with antipsychotic drugs. Symptoms include fever, muscle rigidity, altered mental abilities, irregular pulse and blood pressure, increased heart rate, sweating, and irregular heart rhythm.

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Use only if clearly needed and the potential benefits out- weigh the possible hazards to the fetus.

Breastfeeding: It is not known if these drugs appear in breast milk. Consult your doctor before you begin breastfeeding.

Children: Safety and effectiveness of help have not been established. Safety and effectiveness of pimozide in children younger than 12 years of age have not been established.

Elderly: A lower starting dose is recommended for elderly patients.

Drug Interactions:

Tell your doctor or pharmacist if you are taking or planning to take any over the-counter or prescription medications or dietary supplements with these drugs. Doses of one or both drugs may need to be modified or a different drug may need to be prescribed. The following drugs and drug classes interact with these drugs:

  • Alcohol amphetamines (eg, dextroamphetamine) (pimozide only)
  • Antiarrhythmic agents (eg, quinidine) (pimozide only)
  • Azole antifungals (eg, fluconazole) (pimozide only)
  • Blood pressure-lowering medicines (eg, clonidine)
  • Carbamazepine (eg, Tegretol)
  • Clozapine (eg, Clozaril)
  • Dopamine (eg, Intropin)
  • Fluoxetine (eg, Prozac)
  • Levodopa (eg, Larodopa)
  • Macrolide antibiotics (eg, clarithromycin) (pimozide only)
  • Methylphenidate (eg, Ritalin) (pimozide only)
  • Nefazodone (Serzone) (pimozide only)

Side Effects:

Every drug is capable of producing side effects. Many patients experience no, or minor, side effects. The frequency and severity of side effects depend on many factors including dose, duration of therapy, and individual susceptibility. Possible side effects include:

Digestive Tract: Constipation; dry mouth; diarrhea; nausea; indigestion; vomiting; stomach pain; decreased or increased saliva; toothache; appetite changes.

Nervous System: Tremor; restlessness; headache; dizziness; sleepless­ness; agitation; anxiety; drowsiness; aggressive reaction; increased sleep duration; increased dream activity; nervousness; depression; excitement.

Respiratory System: Upper respiratory infection; sinus irritation; congested or runny nose; coughing; sore throat; difficulty breathing.

Urinary and Reproductive Tract: Frequent urination; heavy menstrual bleeding; difficulty with orgasm; vaginal dryness; difficulty with erection; decreased sexual desire; impotence; lactation; breast enlargement.

Skin: Rash; dry skin; excessively oily skin; dark spots on the skin; sensitivity to sunlight; hair loss.

Other: Fast heartbeat; back, chest, or joint pain; muscle stiffness or rigidity; difficult or abnormal movement; clumsiness; difficulty walking; involuntary muscle contractions; fatigue; dizziness or light-headedness upon rising or standing; visual changes; weight gain; fever; sweating.

Guidelines for Use:

  • Dosage is individualized. Take exactly as prescribed.
  • Do not stop taking or change the dose, unless instructed by your doctor.
  • Can be taken with or without food. Take with food if stomach upset occurs. Avoid grapefruit juice while taking pimozide.
  • Generally, low starting doses are used and then the dose is increased to achieve the best effects.
  • Contact your doctor immediately if you experience skin rash, sexual days function, difficulty breathing, involuntary muscle movements, muscle rigidity, fever, irregular or fast heartbeat, or profuse sweating.
  • May cause dizziness, light-headedness, or fainting when rising or standing, particularly during initial use. Get up slowly and avoid sudden changes in posture.
  • May cause drowsiness. Use caution while driving or performing other tasks requiring alertness, coordination, and physical dexterity.
  • Avoid alcohol while you are taking this medicine.
  • May cause sensitivity to sunlight. Avoid prolonged exposure to the sun or other forms of ultraviolet (UV) light (eg, tanning beds). Use sunscreens and wear protective clothing.
  • Consult your doctor or pharmacist before taking prescription or OTC drugs or dietary supplements with phenylbutylpiperadine derivatives.
  • Inform your doctor if you are pregnant, become pregnant, are planning to become pregnant, or are breastfeeding.
  • Store tablets at controlled room temperature (59 to 86°F) in a tightly closed container and protect from light. Store oral solution at controlled room temperature (59 to 86°F) and protect from light. Do not freeze.

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