An adult should consume at least 10-11 mg of zinc every day. But when taken with food, no more than 40% of this microelement is absorbed. Therefore, in some cases, additional use of drugs containing zinc, for example, Zincorol, is required. This is an effective remedy that can be purchased at an affordable price in pharmacy chains without a doctor's prescription.
pharmachologic effect
Melatonin is a synthetic analogue of a hormone that is produced by the pineal gland and has a chemical structure similar to serotonin . Physiological conditions promote the secretion of melatonin , which increases immediately with the onset of the dark period of the day. Secretion reaches its maximum from approximately 2 to 4 am, and a decrease occurs in the second half of the night. Melatonin is known to be able to control circadian rhythms and sense the day-night cycle. Melatonin has a strong hypnotic effect and helps you fall asleep quickly.
This effect is achieved due to the fact that melatonin affects the MT1, MT2 and MT3 receptors, and it is these receptors that play a significant role in the regulation of circadian rhythms. It has been proven that with age, the content of this substance in the body decreases significantly, so Circadin is very popular among the older generation (over 55 years old) and people who suffer from primary insomnia .
When taking 2 mg of Circadin per day in the afternoon, patients already from the first days of taking it note that the duration of sleep increases and the quality of sleep improves. Many patients also say that with constant use of the drug, not only sleep improves, but also activity during wakefulness, and there is no deterioration in psychomotor reactions throughout the day.
Pharmacology
Zinc is one of the vital elements; the body needs its regular supply from the first to the last days of life. This is an essential microelement, and the total zinc content in an adult reaches 2 g. The indicator may vary depending on gender, age and characteristics of the body.
Zinc performs quite a few functions in the body:
- takes part in the work of 300 enzymes;
- participates in the formation of DNA and RNA;
- takes part in the immune response;
- ensures normal brain function;
- increases performance;
- helps improve memory;
- ensures growth processes, which is especially important for children and adolescents;
- prevents cell damage from free radicals, acts as an antioxidant;
- participates in the absorption of fatty acids and vitamin A;
- ensures healthy skin, nail plates and hair.
Pharmacodynamics and pharmacokinetics
Suction
When taking melatonin orally, it has been determined that in adults this substance is quickly and without any problems absorbed into the gastrointestinal tract, but in older people the rate of absorption of the drug can decrease by 40-50%.
If the dose range when taking melatonin is from 2 to 8 mg, then the kinetic parameters do not lose the linear nature of the dynamics. The bioavailability of Circadin is about 15%. Please note that during the studies, a significant effect of the so-called “first pass” was noted, with estimates of primary metabolism reaching 80-85%. TCmax is fixed at 3 o'clock. It is also noted that food intake can have a strong effect on both melatonin and plasma Cmax. When taking food and Circadin tablets at the same time, the absorption of melatonin slows down and this can lead not only to a rather late TCmax, but also to a lower Cmax.
Distribution
During in vitro studies, it was determined that the binding of the active substance to blood plasma proteins reaches 60%. The strongest association of melatonin occurs with albumin, HDL (high density lipoprotein), and alpha1-acid glycoprotein.
It has been proven that with long-term treatment the drug does not accumulate. This is due to the fact that the T1/2 of melatonin in humans is very short. After 1 and 3 weeks of continuous treatment with this sleeping pill, 2 hours after taking the tablet (at approximately 23:00), a blood draw was taken, as a result of which its concentration was determined. It was 431±83.1 pg.
Metabolism
Experimental studies have suggested that isoenzymes such as CYP1A1, CYP1A2, and CYP2C19 contribute metabolism of melatonin The main metabolite of melatonin is the inactive 6-sulfatoxymelatonin. First-pass metabolism occurs in the liver, and complete excretion of the metabolite ends approximately 12 hours after taking Circadin.
Removal
T1/2 of Circadin reaches 3-3.5 hours. The kidneys play a major role in excretion of the drug (89% in the form of conjugates of 6-hydroxymelatonin glucuronide and sulfate). The rest of Circadin is excreted unchanged from the human body.
Pharmacokinetics in special clinical situations
Please note that the Cmax of the drug in women can increase 3-4 times compared to the values recorded in men.
Due to the fact that the metabolic in older patients (55-68 years old); strongly slows down with age, then their AUC and Cmax values are higher (AUC can reach 5000 pg × h/ml, and Cmax - 1200 pg/ml).
Since the liver is the main organ involved in the metabolism of Circadin, serious liver diseases can cause a strong increase in the concentration of melatonin (endogenous). It has been noted that the concentration of melatonin in the blood plasma reaches its maximum during the day and patients with liver cirrhosis need to be as careful as possible at this time. Also, patients with cirrhosis showed a strong decrease in 6-sulfatoxymelatonin excretion when compared with controls.
Zinc-rich foods
The daily requirement of zinc depends on age and gender:
- adult men 11 mg;
- adult women 8 mg;
- pregnant and lactating women 11-12 mg;
- children under 3 years old – 3-5 mg;
- children 4-7 years old 6-8 mg;
- children 8-18 years old 10-12 mg (increased need is associated with intensive development during adolescence).
Zinc comes from both animal and plant foods:
- cereals;
- legumes;
- oilseeds;
- cereals;
- pumpkin (seeds);
- pork;
- beef;
- crabs;
- yogurt;
- lobsters.
At the same time, oysters are the absolute champion in terms of the content of this microelement. It is important to understand that even with a balanced diet, zinc deficiency cannot be ruled out. The fact is that only 20-40% of it is absorbed from foods. Therefore, in some cases it is necessary to use additional sources, including Zincorol tablets.
It is worth remembering that some foods, such as alcoholic drinks, coffee and tea in excessive quantities, deplete zinc reserves and interfere with its normal absorption. Therefore, while taking Zincorol, it is recommended to avoid drinking these drinks.
Contraindications
It is not recommended to use the drug Circadin:
- with congenital galactose intolerance ;
- in the presence of glucose-galactose malabsorption syndrome ;
- with congenital lactose deficiency ;
- for autoimmune diseases ;
- for renal failure ;
- with liver failure ;
- during pregnancy ;
- during lactation (during breastfeeding);
- under the age of 18;
- in case of hypersensitivity to any of the components of the drug.
"Zinkorol": description, composition
The drug is not a medicine; it belongs to the group of dietary supplements to the basic diet. Used to replenish zinc deficiency in a conveniently digestible form.
The product is produced in the form of tablets, which contain the main component – zinc in the form of organic citrate salt. Additional components are also present.
The drug is stored in standard room conditions at temperatures up to 25 degrees Celsius. Avoid exposure to sunlight and keep away from children. The general shelf life is 3 years from the date of production, subject to storage rules.
Side effects
While taking the drug Circadin, patients may experience discomfort:
From the cardiovascular system: from hot flashes (periodic redness of the facial skin).
From the digestive system: abdominal pain, constipation, dry mouth, digestive disorders and disorders, vomiting, increased intestinal motility, flatulence, hyperproduction of the salivary gland, bad breath .
From the skin: from hyperhidrosis, eczema, erythema, itchy rash and itching, dry skin, nail damage, night sweats.
From the side of the central nervous system: irritability, excitability, fatigue, insomnia, pathological dreams, migraines, psychomotor hyperactivity, dizziness, drowsiness, mood swings, aggressive behavior, agitation, tearfulness, early morning awakening, increased libido, memory impairment, decreased concentration, poor quality of sleep.
From the organ of vision: from decreased visual acuity, blurred vision, increased lacrimation .
From the organ of hearing and labyrinthine disorders: from dizziness when changing body position.
Laboratory indicators: leukopenia and thrombocytopenia, hyperbilirubinemia, hypertriglyceridemia, increased activity of liver transaminases, changes in laboratory indicators of liver function .
Other: from asthenia, weight gain, muscle cramps, neck pain, priapism, fatigue, shingles, edema .
Overdose
To date, not a single case of overdose with the drug Circadin has been recorded. During the studies, a group of subjects used Circadin at a dose of 5 mg per day for about 12 months. As a result, none of the subjects showed any changes or serious side effects. It has been proven that when using the sleeping pill Circadin in a daily dose in the range of 200-300 mg, it does not cause any clinically significant side effects.
A possible reaction in case of overdose may be the development of severe drowsiness , but since the clearance of the active substance varies within 12 hours, this symptom will completely disappear 10-12 hours after taking the sleeping pill orally. Special treatment for overdose is not required.
Interaction
Pharmacokinetic interaction
It has been proven that when taking the drug Circadin in concentrations that significantly exceed therapeutic doses, melatonin is able to induce CYP3A in vitro. To date, experts have not yet identified the clinical significance of this fact and therefore advise, if signs of induction develop, to discuss with your doctor the issue of reducing the doses of drugs that are used simultaneously with sleeping pills.
Even at high concentrations, melatonin does not tend to induce CYP1A enzymes in vitro. Thus, its interaction with other active substances is likely but minimal.
This sleeping pill should be taken with extreme caution by patients who are already using a drug such as fluvoxamine , since it is this drug that, when taken together, can cause a strong increase in melatonin . During the experiment, it was determined that fluvoxamine can provoke an increase in AUC by 15-17 times, and Cmax in the blood by 10-12 times. This effect is achieved due to the process of inhibition of melatonin metabolism by such cytochrome as P450 (CYP) - CYP1A2 and CYP2C19.
Caution should also be exercised in patients taking 5- or 8-methoxypsoralen. This substance can also cause an increase in melatonin concentrations as a result of the process of inhibiting metabolism. of melatonin increased by the combined use of cimetidine (a CYP2D inhibitor), which also affects the inhibition process.
Please note that smoking reduces melatonin concentrations due to stimulation of CYP1A2. estrogens ( contraceptives or hormone replacement therapy), which also cause an increase in melatonin concentrations, should also consult their doctor
quinolones may be responsible for significantly increased melatonin exposure . Inducers of CYP1A2 ( carbamazepine, rifampicin ) can reduce the concentration of the active substance in the blood plasma.
Studies on the interaction of Circadin and inhibitors of prostaglandins, benzodiazepines, agonists, antagonists , as well as antidepressants , tryptophan and ethanol have not yet been carried out, but in the modern scientific literature there are many examples that relate to the effect of these substances on the secretion of melatonin .
Pharmacodynamic interaction
Experts advise that during the course of taking this sedative, you should completely abstain from drinking alcohol , since when taken together, the effectiveness of the drug is greatly reduced.
Circadin can greatly increase the sedative effects of both benzodiazepine and non-benzodiazepine hypnotics. It is better to avoid taking Circadin and Zaleplon, Zolpidem and Zopiclone , since the combination of these drugs can cause a progressive disorder of both attention, memory and coordination.
The combined administration of Circadin with drugs that affect the central nervous system ( Thioridazine, Imipramine ) can increase feelings of calm and provoke serious difficulties in performing certain tasks.
You should also avoid taking it together with NSAIDs.
Reviews about Circadin
The average rating of Circadin on the forums is 4.6 on a 5-point scale.
Forum visitors include the following advantages of the drug:
- soft action;
- no aftereffect;
- maintaining the effect after the course.
Discussants consider the following to be a disadvantage of the drug:
- high cost.
After analyzing the reviews about Circadin on the forums, we can conclude that it is most often used by older people to get rid of primary insomnia.
There is no information about the drug Circadin on Wikipedia.
Indications
The drug is indicated for use in the presence of signs of zinc deficiency:
- problems with growth, including at the stage of intrauterine development (decreased height and weight);
- problems with the immune system (diarrhea, frequent pneumonia);
- complications during pregnancy (intrauterine development abnormalities and premature birth may occur);
- macular degeneration (decrease in central vision due to age-related reasons).
There are also nonspecific signs that may indicate a lack of zinc in the body:
- problems sleeping, insomnia;
- poor skin condition;
- brittle nails;
- weak appetite;
- hair loss;
- mood swings, depression;
- long-term non-healing wounds.
Circadin price, where to buy
The average retail price of Circadin in Ukraine is 540 UAH.
You can buy the medicine Circadin in Moscow for 640 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Circadin tablets prolonged action 2 mg 21 pcs. SwissCo Services AG CH
RUB 851 order
