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Title : Antiarrhythmics-Food Interactions
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Antiarrhythmics-Food Interactions

The interaction between drugs and certain foods can have a significant impact on the therapeutic efficacy of drugs as well as an impact on the profile of adverse effects of a wide range of drugs. Clinical significance of drug-food interactions can be variable and meaningful.

The effect from interaction with food may result in reduced bioavailability of the drug, but also it can change the clearance of the drugs. Thus, some drugs will reach toxic plasmatic levels resulting in serious adverse effects, even death, while others won’t be in the therapeutic range leading to therapeutic failure. The food and specific nutrients that are an integral part of it, ingested simultaneously with certain drugs can affect the overall bioavailability, pharmacokinetics, pharmacodynamics and therapeutic efficacy of drugs. In other words, the presence or absence of certain nutrients in the gastrointestinal tract and/or in a physiological system in the body such as blood can worsen or improve the rate of absorption and metabolism of the drug. The fact is that drug-food interactions may occur with prescribed drugs, but also with OTC preparations including vitamins and minerals.

It is also important to mention that, in some cases, drug-food interactions can have beneficial effects that are evident in the increase of efficacy or reduction of potential side effects.

Therefore, pharmacists in everyday practice must be careful in how they monitor potential drug-food interactions and advise patients which food or drink should be avoided during administration of appropriate therapy drug. In fact these tips above should be allocated to patients who belong to the domain of high-risk patients or patients with diabetes, hypertension, depression, high cholesterol, congestive heart failure, and older people taking three or more drugs that are part of chronic.

Factors affecting the level of drug-food interactions

The following factors have effect on the seriousness of the interactions: the dose of drug that is administered, the age and condition of the patient. In addition, the timing of taking the drugs and foods that are consumed are also factors that play an important role. But to prevent and avoid any drug-food interactions, it does not necessarily mean avoiding certain medications and food. In fact it’s only taking them at suitable intervals, 1 hour before or 2 hours after a meal, rather than eliminating a particular drug or food.

Antiahrrytmics-food interactions

Lidocaine

There are documented drug-food interactions associated with lidocaine, which must taken into account. Lidocaine, a drug from group IB Class I antiarrhythmic drugs is subject to hepatic first-pass metabolism, so its bioavailability is significantly increased when taken with food. Certain studies have shown that hepatic clearance of lidocaine increases from 1,245 to 1,477 ml / min after ingestion of food. It was also shown that dietary protein does not affect the transport of the drug in blood circulation. This is explained with the fact that the increased hepatic clearance is due to increased blood flow in the liver stimulated by ingested food. This is due to the saturation of the enzymes that are responsible for clearance of lidocaine, resulting in its increased bioavailability when the drug is taken orally with food.



 Propafenone

– In the case of propafenone, a drug from group class IC antiarrhythmics, increased bioavailability is also associated with food intake. Propafenone is subject to first-pass metabolism. In this regard there are two distinct phenotypes to be considered, known as slow and fast metabolisers. When comparing the bioavailability of propafenone taken on an empty stomach and after meals, an increase in peak plasma concentrations that are achieved faster is when the drug is taken with food. With the exception of cases of slow metabolisers, there is an increase in area under the curve that can reach 150% when the drug is taken with breakfast. In the case of slow metabolisers, the food does not affect bioavailability. The difference is actually due to the effects of increased blood flow related to food intake. In slow metabolisers, slow hepatic metabolism makes a similar outcome with and without food because most of the drug reaches into circulation without being metabolized in the liver.



Flecainide

In the case of flecainide, another drug from the IC group, t elimination of unchanged drug in urine approximately 27% has been established. In that regard, urinary elimination is reduced in patients who have diets alkalize the urine. Reduced absorption of flecainide is observed when consumed with milk and consequently may lead to increased risk of toxicity when removing milk from the diet.

Beta blockers

 In class II antiarrhythmics, beta blockers, interactions with certain foods is also observed. Availability of bevantolol is not affected when taken with food, while absorption and maximum plasma concentration of acebutolol and its main metabolite diacetolol is reduced without clinical significance. The bioavailability of metoprolol is increased when applied with a diet rich in protein. Amino acids reduce the maximum speed of elimination (Vmax) of metoprolol and its metabolites α-hydroxy-metoprolol and O-dimethyl-metorpolol, thus increasing their bioavailability. The mechanisms responsible for this phenomenon include enzymatic inhibition of amino acids (reduction of first-pass metabolism) and limiting the co-substrate (NADPH or oxygen). Neither bioavailability or absorption is not compromised when used with modified-release dosage forms of metoprolol. Same is the case with propranolol, bioavailability is not compromised when using forms with modified release. But differences arise depending on the composition of the diet.

 Thus, a diet rich in protein results in increased bioavailability due to the inhibitory effect of amino acids on hepatic enzyme system, while a diet rich in carbohydrates and low in protein does not affect the bioavailability of propranolol. Some studies have shown that malto-oligosaccharides delay the transport of propranolol. Pectins have a similar effect by reducing its esterification. Exposure to food (seeing or smelling without it to be consumed) in animal and human studies have shown that can increase the bioavailability of propranolol. Regardless of the specific content of the diet, it is noted that the application of propranolol with food may result in increased bioavailability of up to 50% due to saturation of first pass-metabolism. Additionally, in some animal studies has been shown consumtion  of garlic (Allium sativum) may increase the bioavailability of propranolol. On the other hand bioavailability of timolol is not changed when the drug is administered with food.

Ca-channel blockers

Felodipine, antiarrhythmic Class IV, has delayed absorption when applied in dosage forms with continuous release with foods that is associated with an increased retention of the drug in the stomach. Verapamil shows faster absorption when taken with food and used dosage forms continuously release. Additionally there were no changes in the bioavailability of verapamil when taken with foods rich in protein. The use of sustained-release capsules compared to dispersion of the capsule contents in foods does not show significant differences in the pharmacokinetics of verapamil.



Digoxin

The bioavailability of digoxin an inhibitor of Na + / K + ATP-ase may vary depending on the ingested food. A comparative study between digoxin and beta-methyl-digoxin showed higher maximum serum concentrations when the drug is taken in the fasted state than when taken with food, but this difference was significant only in the case of beta-methyl-digoxin.






Source: http:www.healthscopers.com

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