ProHealth health Vitamin and Natural Supplement Store and Health
Home  |  Log In  |  My Account  |  View Cart  View Your ProHealth Vitamin and Supplement Shopping Cart
800-366-6056  |  Contact Us  |  Help
Facebook Google Plus
Fibromyalgia  Chronic Fatigue Syndrome & M.E.  Lyme Disease  Natural Wellness  Supplement News  Forums  Our Story
Store     Brands   |   A-Z Index   |   Best Sellers   |   New Products   |   Deals & Specials   |   Under $10   |   SmartSavings Club

Trending News

Is a Good Night's Sleep at the Top of Your Wishlist?

Ashwagandha Helps Hormones - Aids Arthritis

Why You Should Be Eating More Porcini Mushrooms

A Breathalyzer for Disease?

How Bacopa Can Help Improve Your Cognitive Function

Magnesium Reduces Diabetes and Helps Keep You Young

Lavender Aromatherapy Can Ease Pre-Op Anxiety

Give Your Health a Much-Needed Boost With Geranium

The Role of Resveratrol in Achieving Optimal Health

Could Coconut Oil Help Reduce Antibiotics?

 
Print Page
Email Article

The effect of food and time of administration on the pharmacokinetic and pharmacodynamic profile of metrifonate.

  [ 29 votes ]   [ Discuss This Article ]
By Heinig R, Sachse R • www.ProHealth.com • September 1, 1999


OBJECTIVE: Metrifonate--via its pharmacologically active metabolite DDVP--is an inhibitor of cholinesterase effective in the treatment of Alzheimer's disease. Two separate studies were performed to investigate the influence of food and time of administration, respectively, on the concentration vs. time profiles of metrifonate and DDVP and cholinesterase inhibition.

METHODS: In study I, a single dose of metrifonate 50 mg tablet was administered either in the fasting condition or within 5 min after completion of an American breakfast. In study II, a single dose of metrifonate 80 mg tablet was given either at 8:00 a.m. after overnight fasting, 7:00 p.m. (7 h after lunch) or 10:00 p.m. (4 h after dinner). Both studies were performed in a non-blind, randomized, single-centre, cross-over design in healthy Caucasian volunteers. AUC and Cmax of metrifonate and DDVP as primary parameters were compared between treatments by ANOVA and acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition vs. time profiles were assessed.

RESULTS: In study I a high-fat/high-calorie breakfast had no effect on the AUC of DDVP, while its Cmax was decreased to 56% and tmax was prolonged, compared to the fasting condition. The effects on metrifonate were similar. In study II bioequivalence was shown for AUC and Cmax of DDVP when comparing administration of metrifonate at 8:00 a.m. and 7:00 p.m. Administration at 10:00 p.m. also had no effect on AUC of DDVP while a reduction in rate of absorption was observed. In both studies the equivalence in AUC of DDVP was paralleled by equivalent effects on BChE inhibition. Following single metrifonate administration little inhibition of AChE was observed. Metrifonate was well tolerated.

CONCLUSIONS: Delayed gastric emptying is likely to cause the reduced rate of absorption of metrifonate with food. In view of unchanged bioavailability of its active metabolite, this food effect is considered to be without clinical relevance and metrifonate can be administered with or without food. The decrease in rate of absorption following administration of the drug at 10:00 p.m. is either a protracted food effect or an effect of time. As the bioavailability of DDVP as well as pharmacodynamic profiles were independent of the time of administration it is concluded that metrifonate can be taken in the morning or evening without compromising its safety or efficacy.

Source: J Clin Pharmacol Ther 1999 Sep;37(9):456-64
PMID: 10507245, UI: 99435079

(Institute of Clinical Pharmacology, Wuppertal, Germany. )




Post a Comment

Featured Products From the ProHealth Store
Mitochondria Ignite™ with NT Factor® Vitamin D3 Extreme™ Optimized Curcumin Longvida®


Article Comments



Be the first to comment on this article!

Post a Comment


 
Optimized Curcumin Longvida with Omega-3

Featured Products

Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium
Vitamin D3 Extreme™ Vitamin D3 Extreme™
50,000 IU Vitamin D3 - Prescription Strength
Energy NADH™ 12.5mg Energy NADH™ 12.5mg
Improve Energy & Cognitive Function
Optimized Curcumin Longvida® Optimized Curcumin Longvida®
Supports Cognition, Memory & Overall Health

Natural Remedies

Strengthen Cell Function with Energy-Boosting Niagen Strengthen Cell Function with Energy-Boosting Niagen
Can Autoimmune Conditions be Reversed? Researchers Make a Surprising Discovery Can Autoimmune Conditions be Reversed? Researchers Make a Surprising Discovery
Magnesium + Malic Acid: One-Two Punch for Pain & Fatigue Magnesium + Malic Acid: One-Two Punch for Pain & Fatigue
Nutrients to Combat the Modern Stress Epidemic Nutrients to Combat the Modern Stress Epidemic
Green Coffee Extract: Unique Obesity Intervention Green Coffee Extract: Unique Obesity Intervention

CONTACT US
ProHealth, Inc.
555 Maple Ave
Carpinteria, CA 93013
(800) 366-6056  |  Email

· Become a Wholesaler
· Vendor Inquiries
· Affiliate Program
SHOP WITH CONFIDENCE
Credit Card Processing
SUBSCRIBE TO OUR NEWSLETTERS
Get the latest news about Fibromyalgia, M.E/Chronic Fatigue Syndrome, Lyme Disease and Natural Wellness

CONNECT WITH US ProHealth on Facebook  ProHealth on Twitter  ProHealth on Pinterest  ProHealth on Google Plus

© 2017 ProHealth, Inc. All rights reserved. Pain Tracker App  |  Store  |  Customer Service  |  Guarantee  |  Privacy  |  Contact Us  |  Library  |  RSS  |  Site Map