Nicotinic acid derivatives

• Nicotinic acid (niacin) has proven cholesterol-lowering effects when given in daily doses exceeding 1 gram. However, such doses cause flushing and rashes. Treatment with nicotinic acid should be supervised by a doctor, who can advise on how to increase the dosage over three or four weeks and minimise the risk of side effects.
• Besides nicotinic acid/niacin preparations, there is a nicotinic acid derivative, acipimox (Olbetam). Side effects are less of a problem with this drug, and it may well be the drug of choice if dietary and lifestyle modifications prove ineffective, although safety in long-term use has not been established.

Fibrates
- These drugs can reduce LDL cholesterol levels by as much as 18%, and at the same time raise HDL cholesterol levels.

• – Bezafibrate (Bezalip). Its primary effect is to reduce triglyceride levels. It also increases the breakdown of LDL particles, thus lowering the LDL Cholesterol level in the bloodstream.
• – Clofibrate (Atromid-S) is gradually becoming obsolete. New derivatives have proved just as effective with fewer side effects.
• – Fenofibrate (Lipanthyl) lowers VLDL and LDL cholesterol levels and raises HDL levels.
• – Gemfibrozil (Lopid) reduces VLDL and LDL cholesterol by decreasing the synthesis of VLDL in the liver. It also raises low levels of HDL cholesterol.
• – Ciprofibrate (Modalim) reduces VLDL and LDL cholesterol levels.

The drugs in this group can be used to lower blood cholesterol levels but are more usually given in cases of raised triglyceride levels. Their long-term safety, although not fully established, looks good.

Bile acid sequestrates
Soluble fibre in the diet binds acids in the gut. Some of these bile acids are then excreted and not resorbed in the large intestine as would normally be the case. Cholesterol is then diverted into making more bile acids, thus reducing cholesterol levels. Bile acid sequestrates work in much the same way, but more effectively, binding the acids and then removing them in faeces.

Two bile acid sequestrates widely available are cholestyramine (Questran) and colestipol (Colestid).They are very successful when used correctly, lowering blood LDL levels by as much as 25%, in addition to any impact diet and lifestyle changes might have on blood cholesterol levels. Many patients use them daily to keep cholesterol levels within reasonable limits. The drugs also have the advantage of being confined to the gut; they don’t enter the body.

Bile acid sequestrates can interfere with the functioning of other prescribed drugs, so you should take them at quite different times. The long-term safety of bile-acid sequestrates is well established.

Probucol (Lurselle) has a poorly understood mode of action. It increases the loss of bile acids in faeces, so its effect is similar to the sequestrates. Long-term safety of the drug is not established. It sometimes causes nausea and diarrhoea and is not recommended during pregnancy and breastfeeding.

HMG CoA Reductase Inhibitors
The full term for this group of drugs is 3-hydroxy-3-methyl-glutaryl co-enzyme A reductase inhibitors. Despite the name, the action of these drugs is quite elegant. All body cells synthesise cholesterol; if the blood cholesterol level falls, cholesterol supply to the cells is reduced and the cells try to make up the deficit by stepping up cholesterol synthesis. The cellular manufacture of cholesterol is complex, but one of the key steps is governed by an enzyme called HMG CoA reductase. Block the action of this enzyme and you can block the manufacture of cholesterol in the cells.

Some of the more common inhibitors available are simvastatin (Zocor), pravastatin (Pravachol), fluvastatin (Lescol), atorvastatin (Lipitor) and cerivatatin (Lipobay). These drugs are generally considered the gold standard of lipid lowering therapy with a good record of clinical efficacy and long-term safety.

• 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.

General Information

• Prescribed for treating Uncomplicated urinary infection, Fosfomycin kills a variety of bacteria ( by preventing bacteria from sticking to the wall of the urinary tract and by interfering with bacterial cell division).
• In the body, it is converted to its active form—free fosfomycin.
• Generally, bacteria that are resistant to other antibiotics are not resistant to fosfomycin, so this drug may work where others have failed.

Cautions

Do not take fosfomycin if you are allergic or sensitive to any of its ingredients.

Fosfomycin is meant to be taken once, in a single dose ( Taking more than 1 packet of fosfomycin only increases side effects and it does not improve the drug’s effectiveness by taking more ).

Some less common side effects are :- diarrhea, vaginal irritation, runny nose, nausea, and headache.
Rare Side Effects :- Rare side effects can occur in almost any part of the body. Contact your doctor if you experience any side effect that is unusual, and/or not listed.

Note

• Metoclopramide reduces fosfomycin blood levels.

Usual Dose

• Adult (age 12 and over): 1 packet mixed with water. Child (under age 12) – not recommended.
• Little is known about the effects of fosfomycin overdose. Contact your local healthcare provider for more information.  ALWAYS bring the prescription container when you seek treatment.
• Do not take fosfomycin powder in its dry form. Mix the contents of the packet with 3-4 oz. of cool or cold water until it dissolves. Then drink the solution immediately. You may take fosfomycin with or without food.
• Contact your doctor if your infection does not improve within 2 or 3 days.

For those under Pregnancy/Breast-feeding period

• The safety of using fosfomycin during pregnancy is not known. When this drug is considered crucial by your doctor, its potential benefits must be carefully weighed against its risks.
  It is not known if fosfomycin passes into breast milk.
• Nursing mothers who must take this drug should use infant formula.

Seniors citizen :-

• Seniors may take fosfomycin without special restriction. Consult your doctor when in doubt.