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

Artificial sweeteners linked to risk of weight gain, heart disease and other health issues

All About Ginkgo Biloba: Benefits of This Timeless Herbal Supplement

Yarrow Oil: Here's Why It Deserves a Place in Your First-Aid Kit

Vitamin D supplement use associated with lower risk of breast cancer

Carnitine deficiency suggested as contributor to autism

Lutein — An Important Nutrient for Eye and Brain Health

White Camphor Oil: The Purest Camphor Oil

Taurine: Facts About This Crucial Amino Acid

Lutein, found in leafy greens, may counter cognitive aging

Vitamin D3 Versus D2

 
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
Ultra ATP+, Double Strength Optimized Curcumin Longvida® Mitochondria Ignite™ with NT Factor®


Article Comments



Be the first to comment on this article!

Post a Comment


 
NAD+ Ignite with Niagen

Featured Products

Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils
Optimized Curcumin Longvida® Optimized Curcumin Longvida®
Supports Cognition, Memory & Overall Health
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

Natural Remedies

Relief for Dry, Itchy Skin Caused by Fibromyalgia Relief for Dry, Itchy Skin Caused by Fibromyalgia
Curcumin - a Golden Gift of Nature with Benefits Still Untold Curcumin - a Golden Gift of Nature with Benefits Still Untold
Vital Molecule Increases Cellular Energy and Improves Cognitive Function Vital Molecule Increases Cellular Energy and Improves Cognitive Function
The Guaifenesin Story: A centuries-old bark extract used for clearing the airways – now key to a popular FM symptom-reversal protocol The Guaifenesin Story: A centuries-old bark extract used for clearing the airways – now key to a popular FM symptom-reversal protocol
"It's Not Easy Being Green" - But It Is Healthy

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