Tinidazole over the counter

Tinidazole

Tinidazole is an antibiotic that fights bacteria in the body.

Tinidazole is used to treat certain infections caused by bacteria, such as infection of the intestines or vagina. It is also used to treat certain sexually transmitted infections.

Tinidazole may also be used for purposes other than those listed in this medication guide.

You should not use this medication if you are allergic to tinidazole or metronidazole (Flagyl), or if you are in the first 3 months of pregnancy.

You should not breast-feed a baby while you are taking tinidazole. However, you may begin nursing again 3 days after you take the last dose. Do not keep any milk you collect with a breast pump while you are taking tinidazole.

Before you take tinidazole, tell your doctor if you have kidney disease (or if you are on dialysis), epilepsy or other seizure disorder, a blood cell disorder such as anemia or low platelets, or a weak immune system.

Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Tinidazole will not treat a viral infection such as the common cold or flu.

Do not drink alcohol while taking tinidazole and for at least 3 days after your treatment ends.

A medicine similar to tinidazole has caused cancer in laboratory animals. It is not known if tinidazole would have the same effect in animals, or in humans. Talk with your doctor about your individual risk.

You should not use this medication if you are allergic to tinidazole or metronidazole (Flagyl), or if you are in the first 3 months of pregnancy.

Tinidazole can pass into breast milk and may harm a nursing baby. Do not breast-feed while you are taking tinidazole and for at least 3 days after your last dose.

You may begin nursing again 3 days after your last dose or tinidazole. If you use a breast pump during treatment, throw out any milk you collect while taking tinidazole. Do not feed it to your baby.

To make sure you can safely take tinidazole, tell your doctor if you have any of these other conditions:

  • kidney disease (or if you are on dialysis);
  • epilepsy or other seizure disorder;
  • a blood cell disorder such as anemia or low platelets; or
  • a weak immune system.

FDA pregnancy category C. Do not take tinidazole during the first 3 months of pregnancy. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

A medicine similar to tinidazole has caused cancer in laboratory animals. It is not known if tinidazole would have the same effect in animals, or in humans. Talk with your doctor about your individual risk.

Tindamax

CLINICAL PHARMACOLOGY

Mechanism Of Action

Tinidazole is an antiprotozoal, antibacterial agent. .

Pharmacokinetics

Absorption

After oral administration, tinidazole is rapidly and completely absorbed. A bioavailability study of Tindamax tablets was conducted in adult healthy volunteers. All subjects received a single oral dose of 2 g (four 500 mg tablets) of Tindamax following an overnight fast. Oral administration of four 500 mg tablets of Tindamax under fasted conditions produced a mean peak plasma concentration (Cmax ) of 47.7 (±7.5) μg/mL with a mean time to peak concentration (Tmax) of 1.6 (±0.7) hours, and a mean area under the plasma concentration-time curve (AUC, 0-∞) of 901.6 (± 126.5) μg/hr/mL at 72 hours. The elimination half-life (T1/2) was 13.2 (±1.4) hours. Mean plasma levels decreased to 14.3 μg/mL at 24 hours, 3.8 μg/mL at 48 hours and 0.8 μg/mL at 72 hours following administration. Steady-state conditions are reached in 2½ – 3 days of multi-day dosing.

Administration of Tindamax tablets with food resulted in a delay in Tmax of approximately 2 hours and a decline in Cmax of approximately 10% compared to fasted conditions. However, administration of Tindamax with food did not affect AUC or T1/2 in this study.

In healthy volunteers, administration of crushed Tindamax tablets in artificial cherry syrup, after an overnight fast had no effect on any pharmacokinetic parameter as compared to tablets swallowed whole under fasted conditions.

Distribution

Tinidazole is distributed into virtually all tissues and body fluids and also crosses the blood-brain barrier. The apparent volume of distribution is about 50 liters. Plasma protein binding of tinidazole is 12%. Tinidazole crosses the placental barrier and is secreted in breast milk.

Metabolism

Tinidazole is significantly metabolized in humans prior to excretion. Tinidazole is partly metabolized by oxidation, hydroxylation, and conjugation. Tinidazole is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.

Tinidazole is biotransformed mainly by CYP3A4. In an in vitro metabolic drug interaction study, tinidazole concentrations of up to 75 μg/mL did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.

The potential of tinidazole to induce the metabolism of other drugs has not been evaluated.

Elimination

The plasma half-life of tinidazole is approximately 12-14 hours. Tinidazole is excreted by the liver and the kidneys. Tinidazole is excreted in the urine mainly as unchanged drug (approximately 20-25% of the administered dose). Approximately 12% of the drug is excreted in the feces.

Patients With Impaired Renal Function

The pharmacokinetics of tinidazole in patients with severe renal impairment (CrCL < 22 mL/min) are not significantly different from the pharmacokinetics seen in healthy subjects. However, during hemodialysis, clearance of tinidazole is significantly increased; the half-life is reduced from 12.0 hours to 4.9 hours. Approximately 43% of the amount present in the body is eliminated during a 6-hour hemodialysis session . The pharmacokinetics of tinidazole in patients undergoing routine continuous peritoneal dialysis have not been investigated.

Patients With Impaired Hepatic Function

There are no data on tinidazole pharmacokinetics in patients with impaired hepatic function. Reduction of metabolic elimination of metronidazole, a chemically-related nitroimidazole, in patients with hepatic dysfunction has been reported in several studies .

Microbiology

Tinidazole is an antiprotozoal, antibacterial agent. The nitro- group of tinidazole is reduced by cell extracts of Trichomonas. The free nitro- radical generated as a result of this reduction may be responsible for the antiprotozoal activity. Chemically reduced tinidazole was shown to release nitrites and cause damage to purified bacterial DNA in vitro. Additionally, the drug caused DNA base changes in bacterial cells and DNA strand breakage in mammalian cells. The mechanism by which tinidazole exhibits activity against Giardia and Entamoeba species is not known.

Antibacterial

Culture and sensitivity testing of bacteria are not routinely performed to establish the diagnosis of bacterial vaginosis ; standard methodology for the susceptibility testing of potential bacterial pathogens, Gardnerella vaginalis, Mobiluncus spp. or Mycoplasma hominis, has not been defined. The following in vitro data are available, but their clinical significance is unknown. Tinidazole is active in vitro against most strains of the following organisms that have been reported to be associated with bacterial vaginosis:

Bacteroides spp.
Gardnerella vaginalis
Prevotella spp.

Tinidazole does not appear to have activity against most strains of vaginal lactobacilli.

Antiprotozoal

Tinidazole demonstrates activity both in vitro and in clinical infections against the following protozoa: Trichomonas vaginalis; Giardia duodenalis (also termed G. lamblia); and Entamoeba histolytica.

For protozoal parasites, standardized susceptibility tests do not exist for use in clinical microbiology laboratories.

Drug Resistance

The development of resistance to tinidazole by G. duodenalis, E. histolytica, or bacteria associated with bacterial vaginosis has not been examined.

Cross-resistance

Approximately 38% of T. vaginalis isolates exhibiting reduced susceptibility to metronidazole also show reduced susceptibility to tinidazole in vitro. The clinical significance of such an effect is not known.

Animal Toxicology And/Or Pharmacology

In acute studies with mice and rats, the LD50 for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration. In rats, the LD50 was > 2,000 mg/kg for both oral and intraperitoneal administration.

A repeated-dose toxicology study has been performed in beagle dogs using oral dosing of tinidazole at 100 mg/kg/day, 300 mg/kg/day, and 1000 mg/kg/day for 28-days. On Day 18 of the study, the highest dose was lowered to 600 mg/kg/day due to severe clinical symptoms. The two compound-related effects observed in the dogs treated with tinidazole were increased atrophy of the thymus in both sexes at the middle and high doses, and atrophy of the prostate at all doses in the males. A no-adverse-effect level (NOAEL) of 100 mg/kg/day for females was determined. There was no NOAEL identified for males because of minimal atrophy of the prostate at 100 mg/kg/day (approximately 0.9-fold the highest human dose based upon plasma AUC comparisons).

Clinical Studies

Trichomoniasis

Tinidazole (2 g single oral dose) use in trichomoniasis has been well documented in 34 published reports from the world literature involving over 2,800 patients treated with tinidazole. In four published, blinded, randomized, comparative studies of the 2 g tinidazole single oral dose where efficacy was assessed by culture at time points post-treatment ranging from one week to one month, reported cure rates ranged from 92% (37/40) to 100% (65/65) (n=172 total subjects). In four published, blinded, randomized, comparative studies where efficacy was assessed by wet mount between 7-14 days post-treatment, reported cure rates ranged from 80% (8/10) to 100% (16/16) (n=116 total subjects). In these studies, tinidazole was superior to placebo and comparable to other anti-trichomonal drugs. The single oral 2 g tinidazole dose was also assessed in four open-label trials in men (one comparative to metronidazole and 3 single-arm studies). Parasitological evaluation of the urine was performed both pre- and post-treatment and reported cure rates ranged from 83% (25/30) to 100% (80/80) (n=142 total subjects).

Giardiasis

Tinidazole (2 g single dose) use in giardiasis has been documented in 19 published reports from the world literature involving over 1,600 patients (adults and pediatric patients). In eight controlled studies involving a total of 619 subjects of whom 299 were given the 2 g × 1 day (50 mg/kg × 1 day in pediatric patients) oral dose of tinidazole, reported cure rates ranged from 80% (40/50) to 100% (15/15). In three of these trials where the comparator was 2 to 3 days of various doses of metronidazole, reported cure rates for metronidazole were 76% (19/25) to 93% (14/15). Data comparing a single 2 g dose of tinidazole to usually recommended 5-7 days of metronidazole are limited.

Intestinal Amebiasis

Tinidazole use in intestinal amebiasis has been documented in 26 published reports from the world literature involving over 1,400 patients. Most reports utilized tinidazole 2 g/day × 3 days. In four published, randomized, controlled studies (1 investigator single-blind, 3 open-label) of the 2 g/day × 3 days oral dose of tinidazole, reported cure rates after 3 days of therapy among a total of 220 subjects ranged from 86% (25/29) to 93% (25/27).

Amebic Liver Abscess

Tinidazole use in amebic liver abscess has been documented in 18 published reports from the world literature involving over 470 patients. Most reports utilized tinidazole 2 g/day × 2-5 days. In seven published, randomized, controlled studies (1 double-blind, 1 single-blind, 5 open-label) of the 2 g/day × 2-5 days oral dose of tinidazole accompanied by aspiration of the liver abscess when clinically necessary, reported cure rates among 133 subjects ranged from 81% (17/21) to 100% (16/16). Four of these studies utilized at least 3 days of tinidazole.

Bacterial Vaginosis

A randomized, double-blind, placebo-controlled clinical trial in 235 non-pregnant women was conducted to evaluate the efficacy of tinidazole for the treatment of bacterial vaginosis. A clinical diagnosis of bacterial vaginosis was based on Amsel’s criteria and defined by the presence of an abnormal homogeneous vaginal discharge that (a) has a pH of greater than 4.5, (b) emits a “fishy” amine odor when mixed with a 10% KOH solution, and (c) contains ≥ 20% clue cells on microscopic examination. Clinical cure required a return to normal vaginal discharge and resolution of all Amsel’s criteria. A microbiologic diagnosis of bacterial vaginosis was based on Gram stain of the vaginal smear demonstrating (a) markedly reduced or absent Lactobacillus morphology, (b) predominance of Gardnerella morphotype, and (c) absent or few white blood cells, with quantification of these bacterial morphotypes to determine the Nugent score, where a score ≥ 4 was required for study inclusion and a score of 0-3 considered a microbiologic cure. Therapeutic cure was a composite endpoint, consisting of both a clinical cure and microbiologic cure. In patients with all four Amsel’s criteria and with a baseline Nugent score ≥ 4, tinidazole oral tablets given as either 2 g once daily for 2 days or 1 g once daily for 5 days demonstrated superior efficacy over placebo tablets as measured by therapeutic cure, clinical cure, and a microbiologic cure.

Table 2: Efficacy of Tindamax in the Treatment of Bacterial Vaginos is in a Randomized, Double-Blind, Double-Dummy, Placebo-Controlled Trial: Modified Intent-to-Treat Population1 (n=227)

The therapeutic cure rates reported in this clinical study conducted with Tindamax were based on resolution of 4 out of 4 Amsel’s criteria and a Nugent score of < 4. The cure rates for previous clinical studies with other products approved for bacterial vaginosis were based on resolution of either 2 or 3 out of 4 Amsel’s criteria. At the time of approval for other products for bacterial vaginosis, there was no requirement for a Nugent score on Gram stain, resulting in higher reported rates of cure for bacterial vaginosis for those products than for those reported here for tinidazole.

Rising Pheonix
program

Our Children’s program is specifically designed for kids ages 7-12. We help our students set both short term and long term goals and continually work towards achieving those goals. Our curriculum helps children develop and refine their motor skills, as well as exercising to increase speed, power and flexibility. Highkicks students push themselves to become stronger athletes.
While the physical benefits of taekwondo are very great, the mental benefits are just as rewarding. We continually motivate our students to increase their knowledge and willingness to learn. To do this we use the “Black Belt” attitude. The Black Belt attitude teaches students to understand that the path to Black Belt is not one that only happens inside the dojang; it also takes place at your home, at your school and in your community. Every aspect of your life must reflect the Black Belt attitude that the Highkicks Masters expect.
This teaches students to come to class with an open mind, practice hard and leave the dojang knowing that they tried as much as possible to better their skills. While they learn, our students are also expected to help other students in their continual progress. Our children practice 5 different aspects of taekwondo. These include kicking and punching skills, forms (patterns), one-step self-defenses, sparring and breaking.
There is not one area of taekwondo that is more important or outweighs another area; all 5 pillars are very important but all must co-exist equally.

About the author

Leave a Reply

Your email address will not be published. Required fields are marked *