Circulatory failure, or the inability of the heart to provide sufficient cardiac output to sat­isfy tissue metabolic requirements, is the most important and most common cause of altered pharmacokinetics during cardiac emergencies. Circulatory failure may result from decreased myocardial contractility, arrhythmias that allow insufficient time for diastolic filling or impair atrioventricular synchrony, circulatory stresses such as increased afterload or hypovolaemia, valvular dysfunction, tamponade, or a variety of less common insults.

Regardless of the aetiology, circulatory fail­ure elicits characteristic compensatory haemodynamic adjustments, mediated in large part by activation of the sympathetic nervous system [Peniel & Benowitz 1984; Benowitz & Meister 1978]. Enhanced sympathetic tone in­creases cardiac contractility and peripheral vas­cular resistance, both of which serve to main­tain arterial blood pressure. The increase in peripheral vascular resistance, however, is not uniform among different vascular beds.

Organs with high metabolic requirements such as the heart and brain exhibit autoregulation; despite sympathetic stimulation, the vessels in these or­gans remain relatively vasodilated as a result of the local effects of hypoxia, lactic acid or other products of anaerobic metabolism that accu­mulate when organ perfusion is reduced. Blood flow to the heart and brain tends to be pre­served, while vasoconstriction decreases blood flow in other organs such as the skin, muscles, and splanchnic organs.

Pathophysiology of Cardiopulmonary Resuscitation (CPR)

Cardiac output during cardiopulmonary resuscitation (CPR) is severely compromised; in humans the mean arterial pressure is less than 50% of normal (Chandra et al. 1981; McDonald 1981), and cardiac output in dogs is less than 30% of normal (Vorhees et al. 1980). Haemodynamic measurements are difficult to obtain in patients during CPR, but animal data suggest that changes in blood flow distribution are qualitatively similar to those observed with circulatory failure and spontaneous circulation.

Blood flow during CPR in anaesthetised, electrically fibrillated dogs is reduced to all organs, but is least reduced to the brain and next least to the heart (Vorhees et al. 1980). For the purpose of pharmacokinetic considerations, CPR and circulatory failure with spontaneous circulation can be considered to be similar, in that total cardiac output is reduced and the pattern of blood redistribution during promptly initiated CPR resembles that seen in circulatory failure.

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• Angiotensin-Converting Enzyme Inhibitor – Vasotec Enalapril
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• Drugs Usage during Critical Medical Emergencies – Synopsis of Important Principles
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• Cathartics, Enemas and Activated Charcoal
• Treating Diabetes Type2 with Miglitol ( Glyset, Acarbose, Precose )
• Drug Overdosage and Poisoning – Synopsis of Important Principles

• Anxiety,
• tension,
• symptoms of acute alcohol withdrawal,
• partial seizures,
• fatigue,
• agitation,
• irritable bowel syndrome,
• and panic attacks.

General Information of the drug

• Clorazepate dipotassium is a benzodiazepine, which directly affect the brain. This drug is a central-nervous-system depressant, and can relax you and make you more tranquil or sleepier, or they can slow nervous system transmissions in such a way as to act as an anticonvulsant.
• Many doctors prefer benzodiazepines to other drugs that can be used to similar effect because they tend to be safer, have fewer side effects.
• Clorazepate may increase blood levels of digoxin and the chances of digoxin toxicity.
• Don’t mix it with alcohol, other sedatives, narcotics, barbiturates, monoamine oxidase inhibitor and other antidepressants, and antihistamines.
• Taking clorazepate with other similar effects drugs may result in excessive depression, tiredness, sleepiness, breathing difficulties, or related symptoms.
• Combining clorazepate with phenytoin may increase phenytoin blood concentrations and the chances of phenytoin toxicity.
• Smoking may reduce clorazepate’s effectiveness by increasing the rate at which it is broken down by the body.
• Clorazepate’s effects may be prolonged when it is mixed with cimetidine, contraceptive drugs, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, probenecid, propoxyphene, propranolol, rifampin, or valproic acid.
• If you have to take Tranxene for a prolong period of time, your doctor will need to monitor your blood counts and liver function to be sure of your health state.
• Theophylline may reduce clorazepate’s sedative effects.
• If you take antacids, separate them from your clorazepate dose by at least 1 hour to prevent them from interfering with the absorption of clorazepate into the bloodstream.
• The effect of levodopa + carbidopa may be decreased if it is taken together with clorazepate.

Cautions ( This drug may be addictive ! )

• Clorazepate may be addictive. It should be used with caution in people with a history of drug dependence.
• Do not take clorazepate if you are allergic or sensitive to any of its ingredients or to another benzodiazepine drug, including clonazepam.
• Clorazepate can aggravate narrow-angle glaucoma, but you may take it if you have open-angle glaucoma and are receiving therapy for it.
• Clorazepate should not be taken by psychotic patients because it is not effective for them and can trigger unusual excitement, stimulation, and rage.
• Clorazepate is not intended to be used for more than 3-4 months at a time. Your doctor should reassess your condition before continuing your prescription beyond that time.
• Your dosage should always be reduced gradually to prevent drug withdrawal symptoms, which may develop if you stop taking it after as few as 4 weeks of regular use but is more likely after longer use.
• Drug withdrawal symptoms may start with anxiety and progress to tingling in the hands or feet, sensitivity to bright light, sleep disturbances, cramps, tremors, muscle tension or twitching, poor concentration, flu-like symptoms, fatigue, appetite loss, sweating. and changes in mental state.
• Other conditions in which clorazepate should be avoided are: severe depression, severe lung disease, sleep apnea (intermittent cessation of breathing during sleep), liver disease, drunkenness, and kidney disease. In each of these conditions, the depressive effects of clorazepate may be enhanced or could be detrimental to your overall condition.

Note

• This drug is for Adult Only ! It is not recommended for child.
• Clorazepate is best taken on an empty stomach, but if it upsets your stomach then it may be taken with food. Consult your doctor on this.
• Clorazepate can cause tiredness, drowsiness, inability to concentrate, or similar symptoms. Be careful if you are driving, operating machinery, or performing other activities that require concentration.
• People taking clorazepate for more than 3 or 4 months at a time may develop drug withdrawal reactions if the medication is stopped suddenly (see “Cautions” section above). Do not stop taking clorazepate or increase or decrease your dosage without first consulting your doctor.
• Do not take a double dose. If you forget a dose of clorazepate, take it as soon as you remember. If it is almost time for your next dose, skip the dose you forgot and continue with your regular schedule.

Pregnancy/Breast-feeding period :

• Clorazepate may cause birth defects if taken during the first 3 months of pregnancy.
• Avoid this drug if you are or might be pregnant, as Clorazepate may pass into breast milk. Nursing mothers who must take clorazepate should switch to use infant formula.

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• Treatments Usage and Effects of Dronabinol Drug (Or Marinol )
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• Synopsis of Important Principles – Drugs in Anaesthetic Practice
• Drug Overdosage and Poisoning – Synopsis of Important Principles
• Angiotensin-Converting Enzyme Inhibitor – Vasotec Enalapril
• Gastric Aspiration and Lavage

• Nausea and vomiting associated with cancer chemotherapy,
• appetite stimulation and weight-loss prevention in people with acquired immunodeficiency syndrome (AIDS).

General Information

• Dronabinol is a legal form of marijuana. The psychoactive chemical in marijuana is delta-9-THC. Dronabinol has all of the psychological effects of marijuana and is therefore considered to be a highly abusable drug.
• Dronabinol increases the effects of alcohol, sleeping pills, sedatives, and other depressants.
• Dronabinol also enhances the effects of psychoactive drugs including tricyclic antidepressants, amphetamines, cocaine, and other stimulants.
• This drug is known to be potential cause of personality changes, feelings of detachment, hallucinations, and euphoria (feeling “high”).
• Younger adults have reported a greater success rate with dronabinol, probably because they are better able to tolerate these effects.
• Most people start taking dronabinol while in the hospital so their response to the drug and its possible adverse effects can be monitored.
• Dronabinol has also been studied as a glaucoma treatment. ( More information to be researched in this field )
• Dronabinol may increase the effects of fluoxetine and disulfiram.
• The effects of theophylline drugs are reduced by dronabinol.
• Combining dronabinol and antihistamines or anticholinergic drugs may cause either rapid heartbeat or excessive drowsiness.

Cautions ( This drug has serious effects ! )

• Do not take dronabinol if you are allergic or sensitive to any of its ingredients, to marijuana. or to sesame oil.
• Dronabinol should be used with caution in those with a history of seizure disorders or substance abuse.
• Dronabinol should be used with caution by people with heart disease or high blood pressure.
• Dronabinol has a profound effect on mental states, as it will impair your ability to operate complex equipment or engage in any activity that requires intense concentration, sound judgment, or coordination—such as driving a car.
• Dronabinol should not be used to treat nausea and vomiting caused by anything other than cancer chemotherapy.
• Dronabinol produces withdrawal symptoms when the drug is stopped. These may develop within 12 hours of the drug’s discontinuation and include restlessness, sleeplessness, and irritability.
• Within a day after the drug has been stopped, symptoms like stuffy nose, hot flashes, sweating, loose stools, hiccups, or appetite loss may occur. These symptoms usually subside within a few days.
• Dronabinol should be used with caution by people with a manic-depressive or schizophrenic history because it may aggravate the underlying disease.

Note :-

• Avoid alcohol and other central nervous system (CNS) depressants.
• The capsules must be stored in the refrigerator.
• Be careful when driving or performing any task that requires concentration.
  Dronabinol may cause acute psychiatric or psychological side effects. Call your doctor for advise.

Common Side Effects of the drug :-

• drowsiness,
• depression,
• loss of muscle coordination,
• unsteadiness,
• paranoia,
• depersonalization,
• disorientation,
• euphoria,
• dizziness,
• weakness,
• sluggishness,
• nausea and vomiting,
• headache,
• a separation in time and space,
• confusion,
• rapid heartbeat.
• hallucinations,
• memory lapses,
• anxiety,
• muddled thinking,
• perceptual difficulties,
• poor coordination,
• irritability,
• dizziness when rising from a sitting or lying position.

Unlikely Side Effects :-

• difficulty talking or slurred speech,
• facial flushing
• loss of bowel control,
• excessive perspiration,
• fainting,
• diarrhea,
• nightmares,
• ringing or buzzing in the ears,
• muscle pain

Usual Dose Intake ( Do not take a double dose )

1. Antiemetic :

• 5 mg 1-3 hours before starting chemotherapy treatment and repeated every 2-4 hours after treatment, for a total of 4-6 doses a day.
• Dosage may be increased up to 15 mg per dose if needed; psychiatric side effects increase greatly at higher dosages.

2. Appetite Stimulant:

• 2.5 mg before lunch or dinner, or 2.5 mg at bedtime. Dosage may be increased to 20 mg a day.

Over Dosage Effect(s)

• Overdose symptoms may occur at usual dosages or at higher dosages if the drug is being abused.
• The primary symptoms of overdose are the psychological symptoms listed above (see “Side Effects lists above”).
• In some cases, overdose may lead to panic reactions or seizure.

Pregnancy/Breast-feeding period :

• Dronabinol is known to be passes into breast milk. Nursing mothers who must take this drug should use infant formula. Animal laboratory studies have shown adverse effects on the fetus.

• Generalized Anxiety Disorder Treatment with Clorazepate ( Tranxene )
• Using Entacapone in Parkinson’s Disease Treatment
• Treating Diabetes Type2 with Miglitol ( Glyset, Acarbose, Precose )
• Drugs Usage during Critical Medical Emergencies – Synopsis of Important Principles
• Angiotensin-Converting Enzyme Inhibitor – Vasotec Enalapril
• Pathophysiology of Circulatory Failure and Cardiopulmonary Resuscitation
• Anaesthetic Agents – Drugs Used in Anaesthesia
• Symptoms, Types and Treatment Options for Warts
• Synopsis of Important Principles – Drugs in Anaesthetic Practice
• Drug Overdosage and Poisoning – Synopsis of Important Principles

• Hypertension ( high blood pressure ),
• heart failure,
• diabetic kidney disease,
• and heart attack treatment ( when the function of the left ventricle has been affected),
• kidney failure,
• kidney hypertension,
• managing people with a high risk of heart disease,
• chronic kidney disease,
• preventing a second stroke.

General Information of the drug

• Enalapril begins working about 1 hour after you take it and continues to work for 24 hours.
• Enalapril maleate and other ACE inhibitors work by preventing the conversion of a hormone called ‘Angiotensin I‘ to another hormone called ‘Angiotensin II‘ , a potent blood-vessel constrictor. Preventing this conversion relaxes blood vessels, thus reducing blood pressure and relieving symptoms of heart failure.
• Enalapril also affects the production of other hormones and enzymes that participate in the regulation of blood-vessel dilation.

Cautions

• Enalapril occasionally causes very low blood pressure.
• Do not take enalapril if you are allergic or sensitive to any of its ingredients. Severe sensitivity reactions can occur in hemodialysis patients taking enalapril or those undergoing venom immunization.
• Swelling of the face, extremities, or throat has been known to occur with enalapril, which can be dangerous (see below section on “Important Notes” ).
• Enalapril may affect your kidney function, especially if you have congestive heart failure. Your doctor should check your urine for protein content during the first few months of treatment. Dosage adjustment of enalapril is necessary if you have reduced kidney function.
• Enalapril can affect white-blood-cell counts, possibly increasing your susceptibility to infection. Your doctor should monitor your blood counts periodically.
• Enalapril may cause serious injury or death to the fetus if taken during pregnancy. Pregnant women should not take enalapril.
• ACE inhibitors may be less effective in some black patients with high blood pressure, especially when dietary salt intake is high. Nevertheless, they should still be considered useful blood pressure treatments. Swelling beneath the skin to form welts is more common among black patients.

How the Drug works ?

• Antacids and enalapril should be taken at least 2 hours apart.
• The blood-pressure-lowering effect of enalapril is additive with diuretic drugs and beta blockers. Any other drug that causes a rapid drop in blood pressure should be used with caution if you are taking enalapril.
• Enalapril may increase the effects of lithium; this combination should be used with caution.
• Aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) reduce the blood-pressure-lowering effects of enalapril and other ACE inhibitors. The combination may cause reductions in kidney function.
• Enalapril may increase blood-potassium levels, especially when taken with dyazide or other potassium-sparing diuretics.
• Capsaicin may trigger or aggravate the cough associated with enalapril therapy.
• Rifampin may reduce the effects of enalapril.
• The combination of allopurinol and enalapril increases the chance of side effects. Avoid this combination as severe sensitivity reactions can occur in those taking allopurinol.
• Enalapril affects blood levels of digoxin. More digoxin in the blood increases the chance of digoxin-related side effects, while less digoxin in the blood can compromise its effectiveness.
• Indomethacin may reduce the blood-pressure-lowering effects of enalapril.
• Phenothiazine sedatives and antiemetics may increase the effects of enalapril.

Important Note

• Enalapril can cause swelling of the face, lips, hands, or feet. This swelling can also affect the larynx (throat) or tongue and interfere with breathing. If this happens, go to a hospital emergency room at once.
• Call your doctor if you develop a sore throat, mouth sores, abnormal heartbeat, chest pain, persistent rash, or loss of taste perception.
• Some people who start taking enalapril after they are already on a diuretic (an agent that increases urination) could experience a rapid drop in blood pressure after their first doses or when their dosage is increased. To prevent this from happening, inform your doctor before hand ( that you are taking diuretic ) , as your doctor may tell you to stop taking your diuretic 2 or 3 days before starting enalapril or to increase your salt intake during that time. Upon your doctor advise, you may then restart on taking diuretic gradually.
• You may get dizzy if you rise to your feet too quickly from a sitting or lying position when taking enalapril.
• Avoid strenuous exercise or very hot weather because heavy sweating or dehydration can cause a rapid drop in blood pressure.
• While taking enalapril, avoid over-the-counter diet pills, decongestants, and other stimulants that can raise blood pressure.
• Do not take potassium supplements or salt substitutes containing potassium without consulting your doctor.
• Never take a double dose. If you take enalapril once a day and forget to take a dose, take it as soon as you remember. If it is within 8 hours of your next dose, skip the one you forgot and continue with your regular schedule. If you take enalapril twice a day and miss a dose, take it right away. If it is within 4 hours of your next dose, take 1 dose immediately and another in 5 or 6 hours, then go back to your regular schedule.

Possible Side Effects

Refers to Side Effects on Lexxel Drug , as these drugs works in combination in most treatments condition. However, if you experience unusual effects, do consult your doctor for advise.

Pregnancy/Breast-feeding period :

• ACE inhibitors can cause fetal injury or death. Women who are or might become pregnant should not take ACE inhibitors.
• Sexually active women of childbearing age who must take enalapril must use an effective contraceptive method to prevent pregnancy.
• If you become pregnant, stop taking the medication and call your doctor immediately.
• Nursing mothers who must take this drug should use infant formula as small amounts of enalapril pass into breast milk.

For Seniors who needs to take this drug :-

Seniors may be more sensitive to the effects of enalapril drug due to age-related losses in kidney or liver function.

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• Drugs Usage during Critical Medical Emergencies – Synopsis of Important Principles
• Synopsis of Important Principles – Drugs in Anaesthetic Practice
• Treatments Usage and Effects of Dronabinol Drug (Or Marinol )
• Using Entacapone in Parkinson’s Disease Treatment
• Symptoms, Types and Treatment Options for Warts
• Pathophysiology of Circulatory Failure and Cardiopulmonary Resuscitation
• Mupirocin as Topical Antibiotic for Skin Infection

General Information

• Lexxel contains 5 mg of felodipine, a calcium channel blocker, and 5 mg of enalapril, an angiotensin-converting enzyme (ACE) inhibitor. The 2 drugs in this combination belong to widely prescribed groups of hypertension medication.
• Lexxel is not meant for the initial treatment of hypertension.
• Most people taking this product have taken 1 of the ingredients as an individual pill and need more medication to control their blood pressure.
• Felodipine works by blocking the passage of calcium into heart and smooth-muscle tissue, especially the smooth muscle found in arteries. Since calcium is an essential factor in muscle contraction, any drug that affects calcium in this way will interfere with the contraction of these muscles. This causes the veins to dilate (widen), reducing blood pressure. Also, the amount of oxygen used by these muscles is reduced.
• ACE inhibitors such as enalapril work by preventing the conversion of a hormone called angiotensin Ito another hormone called angiotensin II, a potent blood-vessel constrictor. Preventing this conversion relaxes blood vessels and helps to reduce blood pressure and relieve the symptoms of heart failure.
• Enalapril’s effect on other hormones may also help to promote blood-vessel dilation. It begins working about 1 hour after you take it and continues to work for 24 hours.

How does the drug reacts ?

• The blood-pressure-lowering effect of Lexxel adds to that of diuretic (agent that increases urination) drugs or beta blockers.
• Any other drug that causes a rapid blood-pressure drop should be used with caution if you are taking Lexxel.
• When taken with Dyazide or other potassium-sparing diuretics, Lexxel may raise blood-potassium levels.
• Lexxel may increase the effects of lithium; this combination should be used with caution.
• Capsaicin may cause or aggravate the cough associated with Lexxel therapy.
• Nonsteroidal anti-inflammatory drugs (NSAIDs) may interfere with the blood-pressure-lowering effect of Lexxel.
• Phenothiazine sedatives and antiemetics may increase the effects of Lexxel.
• Rifampin may reduce the effects of Lexxel.
• Combining allopurinol with Lexxel increases the risk of an adverse drug reaction.
• Cimetidine, indinavir, nelfinavir, ritonavir, saquinavir, clarithromycin, nefazodone, ketoconazole, itraconazole, erythromycin, telithromycin, aprepitant, fluconazole, and verapamil increase the amount of felodipine in the blood, causing a slight increase in the drug’s effect and possible side effects.
• Phenytoin and other hydantoin anti-seizure drugs, carbamazepine, and barbiturate sleeping pills and sedatives may decrease the amount of felodipine in the blood, reducing its effect.
• Felodipine may increase the effects of theophylline (a drug used to treat asthma and other respiratory problems) and oral anticoagulant (blood-thinning) drugs.
• Felodipine may increase blood levels of tacrolimus. Tacrolimus dose adjustment may be needed.
• Felodipine may interact with quinidine (an antiarrhythmic) to produce low blood pressure, very slow heart rate, abnormal heart rhythms, and swelling in the arms or legs.

Cautions

• Do not take Lexxel if you are allergic or sensitive to any of its ingredients. It could causes very low blood pressure, although rarely occurs.
• Lexxel should be used with caution by people with kidney disease, as it may also affect your kidneys, especially if you have congestive heart failure (CHF). Your doctor should check your urine for protein content during the first few months of treatment.
• Enalapril may affect white-blood-cell counts, possibly increasing your susceptibility to infection. Your doctor should monitor your blood counts periodically.
• ACE inhibitors can cause injury or death to a developing fetus in the last 2 trimesters. Pregnant women should not take Lexxel or any ACE inhibitor.
• People taking a beta-blocking drug who begin taking felodipine may develop heart failure or increased angina pain. Angina pain may also increase if your felodipine dosage is increased.
• People with severe liver disease break down felodipine much more slowly than those with less severe disease or normal livers.
• While taking any ACE inhibitor, sudden and painless swelling in the hands, face, feet, lips, tongue, or throat may develop. If this happens,  stop taking the medication at once , and contact your doctor. This condition usually goes away on its own, though antihistamines may also prove helpful.

Usual Dose and Intakes

• This drug is for adult only.
• 1 tablet a day. ( May be increased to 2 tablets if further blood pressure reduction is necessary after 1-2 weeks of treatment. )
• Overdose may cause low blood pressure. ( In case of overdose, contact your doctor or go to a hospital for emergency attention. ALWAYS bring the prescription bottle or container. )
• Lexxel may be taken without regard to food or meals ( you may take it with food if it upsets your stomach. )
• Avoid grapefruit juice while you are on Lexxel.
• Do not break, crush, or chew Lexxel tablets.
• Maintain good dental hygiene while taking Lexxel and use extra care when brushing or flossing teeth because of the increased risk of oral infection associated with Lexxel.
• Avoid over-the-counter diet pills, decongestants. and stimulants while taking Lexxel; they may raise blood pressure.

Possible Side Effects and Notes

*Side effects are more common with higher dosages and increasing age.
Most common side effects includes :-

• swelling in the ankles, feet, and legs;
• dizziness;
• lightheadedness;
• muscle weakness or cramps;
• facial flushing;
• headache;
• fatigue;
• nausea;
• chronic- (long-term) cough.  ( The cough usually goes away a few days after you stop taking the medication. )

Rare and Less common side effects ( Contact Your Doctor for advise )  :-

• respiratory infection,
• cough,
• tingling in the hands or feet,
• upset stomach,
• abdominal pain,
• chest pain,
• constipation,
• diarrhea,
• heart palpitations,
• sore throat,
• runny nose,
• back pain, rash,
• angina (condition characterized by brief attacks of chest pain),
• vomiting,
• bronchitis,
• urinary tract infection,
• breathing difficulties,
• Unusual condition affecting your heart, muscles and joints, stomach and intestines, sexual function, kidney or liver, and other body parts.

Hypertension may be present without symptoms, thus continue taking your medication and follow any instructions for diet restriction or other treatments to help maintain lower blood pressure, even if you feel well.

Do not take a double dose.

- If you forget a dose, take it as soon as you remember. If it is almost time for your next dose, skip the dose you forgot and continue with your regular schedule.

For those under Pregnancy/Breast-feeding period

Women who are or might be pregnant should not take Lexxel. ACE inhibitors have caused low blood pressure, kidney failure, slow skull formation, and death in the fetus when taken during the last 6 months of pregnancy.

Women of childbearing age who must take Lexxel must use an effective contraceptive method.

If you become pregnant, stop taking the medication and call your doctor immediately.
Nursing mothers who must take Lexxel should use infant formula, as small amounts of enalapril + felodipine are known to pass into breast milk.

Seniors citizen :-

• Especially those with liver disease, may be more sensitive to the drug’s effects. Take it with care., it is best to consult doctor before taking it.

• Angiotensin-Converting Enzyme Inhibitor – Vasotec Enalapril
• Treating Diabetes Type2 with Miglitol ( Glyset, Acarbose, Precose )
• Drugs Usage during Critical Medical Emergencies – Synopsis of Important Principles
• Generalized Anxiety Disorder Treatment with Clorazepate ( Tranxene )
• Using Entacapone in Parkinson’s Disease Treatment
• Amiodarone – Treating Abnormal Heart Rhythms
• Symptoms, Types and Treatment Options for Warts
• Mupirocin as Topical Antibiotic for Skin Infection
• Synopsis of Important Principles – Drugs in Anaesthetic Practice
• Treatments Usage and Effects of Dronabinol Drug (Or Marinol )

Parkinson’s disease

• Chronic (persistent) disorder of part of the brain, which affects the way the brain co-ordinates the movements of the muscles in various parts of the body.

General Information of the drug
Entacapone is always used in combination with levodopa + carbidopa. It is prescribed For Parkinson’s disease patients for whom levodopa + carbidopa loses its effectiveness between doses.

Entacapone enhances the effect of levodopa + carbidopa by reversing the action of an enzyme known as catechol-O-methyltransferase (COMT), which is primarily responsible for breaking down levodopa in the body.

Some patients experience signs and symptoms of an end-of-dose “wearing-off” effect with these drugs.

Cautions

• If you are allergic or sensitive to any of its ingredients -> Do not take entacapone !
• People with liver disease should use entacapone with caution as they may accumulate twice as much of this drug in their blood as people with normal liver function.
• Entacapone may cause kidney toxicity.
• Entacapone may increase the risk of dizziness or fainting when rising from a sitting or lying down position.
• Do not take entacapone with phenelzine or tranyleypromine -> Serious reaction may occur.
• Hallucinations have been reported with other Parkinson’s disease drugs.
• Entacapone has been rarely associated with the formation of fibrous tissues in unusual places such as the urinary tract and lungs. It has also caused fluid in the lungs.

Intake and Dosage

• Adult Dose Intake :- 200 mg with each levodopa + carbidopa dose, up to 1600 mg a day.
• Entacapone may be taken with or without food. However, Do Not Mix entacapone with the monoamine oxidase inhibitor (MAGI) antidepressants phenelzine or tranylcypromine.
• Entacapone may be taken with the MA01 selegiline.
• Other drugs broken down by COMT will also be affected by entacapone.
• lsoproterenol, epinephrine, ephedrine, norepinephrine, isoetharine, and others will interact with entacapone, even when taken by inhalation. The result may be increased heart rate, arrhythmias, and excessive changes in blood pressure.
• Cholestyramine, probenecid, erythromycin, rifampin, ampicillin, and chioramphenicol may interfere with the elimination of entacapone from the body.
• Entacapone may enhance the effects of sedatives and other nervous system depressants.
• Although there have been no reports of significant entacapone overdose as of publcation. But theoretically, a massive entacapone overdose could prove lethal by completely inhibiting COMT throughout the body.
• Doses up to 800 mg have been taken and side effects were mainly abdominal pain and loose stools.
• Other effects that might be expected include difficulty breathing, loss of muscle coordination, reduced level of activity, and convulsions.
• Overdose victims should be taken to a hospital emergency room as soon as possible ( ALWAYS bring along the prescription bottle or container. )
  

Important Note

• This drug can cause dizziness, nausea, sweating, or fainting when rising quickly from a sitting or lying position, especially at the beginning of treatment.
• Always take your entacapone dose together with your levodopa + carbidopa dose. If you forget a dose. take it as soon as you remember. ( If it is within 2 hours of your next dose. skip the dose you forgot and continue with your regular schedule. )
• If you experience an increased body movements and twitching, twisting, or uncontrolled tongue, lip, face, arm, or leg movement, consult your doctor as he may need to adjust your dose of levodopa + carbidopa.
• Until your body has become accustomed to the effects of entacapone, it’s highly advisable to be caution when performing tasks, such as driving, that require coordination and concentration.
• Gradually reducing the dose of entacapone decreases some drug side effects.
• Patients who stop using entacapone should be monitored as rapid withdrawal of the drug can cause high fever, sweating, unstable blood pressure, stupor, and muscular rigidity.
• If your urine to turn a brownish-orange color after taking Entacapone,  it is usually harmless.

Possible Side Effects

Most of the common effects after taking this drugs are :-

• difficulty performing voluntary muscle functions,
• excessive muscle activity,
• nausea,
• urine discoloration,
• diarrhea,
• reduced muscle activity,
• dizziness,
• fatigue,
• constipation,
• abdominal pain.

Less common side effects or rarely occurs side effects ( Consult your doctor immediately ) :-

• low blood pressure and fainting ( especially when rising from a sitting or lying position ),
• hallucinations,
• anxiety,
• agitation,
• gastritis or other stomach disorders,
• dry mouth,
• vomiting,
• increased sweating,
• back pain,
• taste changes,
• shortness of breath,
• easy bruising,
• weakness,
• bacterial infection,
• muscle damage or death,
• high fever,
• confusion.

Pregnancy/Breast-feeding period :

• When this drug is considered crucial by your doctor, its potential benefits must be weighed against its risks.
• Entacapone causes birth defects, miscarriage and abortion in pregnant animals. It has been known that Entacapone passes into the breast milk of animals, but at the moment if publication, there is no information on humans is available. Nursing mothers who must take this drug should use infant formula.

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General Information

• Amiodarone works by decreasing the sensitivity of heart tissue to nervous impulses within the heart. It should be prescribed only in situations where the abnormal rhythm is so severe as to be life-threatening and does not respond to other drug treatments.
• It has not been proven that people taking this drug will live longer than those with similar conditions who do not take it.
• Amiodarone may exert its effects 2-5 days after you start taking it, but often takes 1-3 weeks to affect your heart.
• Amiodarone’s antiarrhythmic effects can last for weeks or months after you stop taking it.

How does the drug Interact ?

• Amiodarone increases the effects of metoprolol and other beta blockers, calcium channel blockers such as verapamil and dittiazem, cyclosporine, dextromethorphan, digoxin, disopyramide, flecainide, fentanyl, lidocaine, methotrexate, procainamide, quinidine, theophylline, and warfarin and other anticoagulants. These interactions can take from 2 or 3 days to several weeks to develop. Some can be life threatening, and for others, drug dosage adjustments may be enough to avoid a serious problem.
• Fluoroquinolones, azole antifungals, and macrolide antibiotics increase the effects of amiodarone. which can cause life-threatening abnormal heart rhythms.
• When amiodarone and phenytoin are taken together, both drugs can be affected. Amiodarone can be antagonized by phenytoin and other hydantoin anticonvulsants, and the effect of phenytoin can be increased by amiodarone.
• Cholestyramine interferes with the absorption of amiodarone into the bloodstream.
• Cimetidine and ritonavir interfere with the breakdown of amiodarone, leading to high drug blood levels and the increased possibility of side effects.
• Azithromycin can interfere with the effectiveness of amiodarone. This interaction may lead to dizziness and cardiac instability.

Cautions ( This drug has fatal effects ! )

• Amiodarone can cause potentially fatal drug side effects too ! At high doses, 10% or more of people taking this drug can develop potentially fatal lung and respiratory effects, beginning with cough and progressive breathing difficulties.
• Do not take amiodarone if you are allergic or sensitive to any of its ingredients or if you have heart block or a very slow heart rate.
• Amiodarone can also cause heart block, a drastic slowing of electrical impulse movement between major areas of the heart, or extreme slowing of the heart rate. Amiodarone heart block occurs about as often as heart block caused by some other antiarrhythmic drugs, but its effects may last longer than those of the other drugs.
• Amiodarone can also worsen existing abnormal heart rhythms in 2-5% of people who take the drug. These effects can be fatal.
• Liver damage caused by amiodarone is usually mild. In rare cases. amiodarone has been associated with liver failure that resulted in death.
• People taking amiodarone may develop optic nerve irritation, leading to partial or complete loss of vision. Most adults who take amiodarone for 6 months or more develop tiny deposits in the corneas of their eyes. These deposits may cause blurred vision or halos in up to 10% of people taking amiodarone. Some people develop dry eyes and sensitivity to bright light.
• One in ten people taking amiodarone can experience unusual sensitivity to the effects of the sun. Use an appropriate sunscreen product and reapply it frequently.
• Amiodarone can cause thyroid abnormalities. It may worsen an already sluggish thyroid gland in 2-10% of people taking the drug, and increase thyroid activity in 2% of people taking it.
• Amiodarone has also been associated with an increase in risk of thyroid tumors.
• Antiarrhythmic drugs are less effective and cause abnormal rhythms if blood potassium is low.

Other Possible Side Effects

• Side effects are very common with amiodarone. About 75% of people taking 400 mg or more of amiodarone a day develop some drug side effects. As many as 18% have to stop taking the drug because of a side effect.
• Amiodarone stays in the body for months, so side effects may remain even after the drug is stopped.
• Unusual sun sensitivity is the most common skin reaction to amiodarone, but people taking this drug can develop a blue skin discoloration that may not go away completely when the drug is stopped.
• Other skin reactions are sun rashes, hair loss, and black-and-blue spots.
• Amiodarone can cause heart failure, reduced heart rate, and abnormal rhythms.
• Up to 9% of people taking amiodarone develop abnormalities in liver function

See your doctor for an eye exam if your vision changes at all while taking amiodarone.

Call your doctor if you develop chest pain. breathing difficulties, spitting up blood, nausea, vomiting, abnormal heartbeat, bloating in your feet or legs. tremors, fever, chills, sore throat, unusual bleeding or bruising, changes in skin color, unusual sunburn, or any other unusual side effect.

Common Side Effects of the drug :-

• fatigue,
• not feeling well,
• tremors,
• unusual involuntary movements,
• loss of coordination,
• an unusual walk,
• muscle weakness,
• low blood pressure,
• dizziness,
• tingling in the hands or feet,
• reduced sex drive,
• sleeplessness,
• headache,
• nervous-system problems,
• nausea,
• vomiting,
• constipation,
• appetite loss,
• abdominal pain,
• dry eyes,
• unusual sensitivity to bright light,
• seeing halos around bright lights.

Rare Side Effects :-

• inflammation of the lung or fibrous deposits in the lungs,
• changes in thyroid function,
• changes in taste or smell,
• bloating,
• unusual salivation,
• changes in blood clotting.

Note

• Amiodarone can make you dizzy or lightheaded. Take care while driving a car or performing complex tasks.
• If you take amiodarone once a day and forget to take a dose, but remember within 12 hours, take it as soon as possible.
• If you do not remember until later, skip the dose you forgot and continue with your regular schedule.
• If you take amiodarone twice a day and remember within 6 hours of your regular dose, take it as soon as you remember.
• Call your doctor if you forget to take 2 or more doses in a row, ask for doctor advise on what to do next – Do not take a double dose.
• Pregnancy and/or Breast-feeding : In high doses, amiodarone has been found to be toxic to animal fetuses. Women of childbearing age should use an effective contraceptive while taking amiodarone. If you are or might be pregnant and this drug is considered crucial by your doctor, its potential benefits must be weighed against its risks.
  Amiodarone passes into breast milk. Nursing mothers who must take this drug should use infant formula.
• Seniors : Dosage reduction may be needed in seniors with poor liver function.

Usual Dose ( Doctor Instruction Should Be followed Closely )

• Starting dose 800-1600 mg a day, taken in 1 or 2 doses, usually for 1-3 weeks. Then, 600-800 mg a day for approximately a month. Maintenance dose 400 mg a day.
• You should take the lowest effective dose in order to minimize side effects.
• Amiodarone should be taken on an empty stomach, as food delays its absorption into your bloodstream.
• If amiodarone upsets your stomach, however, you may take it with food but then always take it with food to be consistent.
• Do not drink grapefruit juice during treatment with amiodarone because grapefruit juice affects how amiodarone is absorbed in the stomach.

Over Dosage Effect(s)

• The effects of amiodarone overdose include low blood pressure. shock, slow heartbeat, and liver toxicity.
• Overdose victims should be taken to a hospital emergency room for treatment.
• ALWAYS bring the prescription bottle or container.

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