Pharmacological properties
Pharmacodynamics.
Metronidazole is a derivative of 5-nitroimidazole, active against anaerobic protozoa and anaerobic bacteria. Metronidazole is effective against trichomonas vaginalis, giardia intestinalis, gardnerella vaginalis, entamoeba histolytica, lamblia spp., as well as obligate anaerobes: bacteroides spp. (b. fragilis, b. distasonis, b. thetaiotaomicron, b. vulgatus, b. ovatus), fusobacterium spp. and some gram-positive microorganisms: eubacterium spp., clostridium spp., peptostreptococcus spp., peptococcus spp. Metronidazole for external use has little antioxidant activity.
It has been established that metronidazole significantly reduces the production of active oxygen, hydroxyl radicals and hydrogen peroxide by neutrophils, which are potential oxidants and can harm tissues at the site of inflammation.
The mechanism of action of metronidazole is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of microorganisms, inhibiting its synthesis, which leads to the death of microorganisms.
When applied topically, the drug is effective against acne, but the mechanism of this action has not been fully studied.
Pharmacokinetics. When used externally, absorption of the drug is minimal and only a small amount of the drug is determined in the blood plasma. Absorbed metronidazole penetrates the placental barrier and the BBB. Cmax in the blood reaches 66 mg/ml (if 1 g of gel is applied, which is equivalent to 7.5 mg of metronidazole).
Sufficient attention to skin hydration
The use of moisturizing creams and such products is mandatory when treating rosacea, as they help relieve the symptoms of the disease. Regular use of a moisturizer suitable for the user's skin type will help significantly reduce itching and unpleasant tingling, as well as prevent burning and tightness of the skin. It is important to purchase a quality product, as there is a risk of worsening the situation and the appearance of new unpleasant symptoms of the disease.
Moisturizing procedures must be done in accordance with the instructions for use of a particular drug. If during use, alarming symptoms arise or the situation worsens, you should stop using the moisturizer and change it to another.
The cream should be used exclusively on clean skin, otherwise the result will be negative. Dirt particles will get lodged in the pores, causing clogging. This is the reason for the appearance of consequences in the form of new rashes and inflammatory processes under the epidermis.
special instructions
Avoid getting the drug into your eyes. If the gel gets into your eyes, you must immediately rinse them with plenty of water.
The gel should not be applied to areas close to the eyes. The affected area should be cleaned before applying Metrogyl gel. After applying the drug, you can use cosmetics.
For ordinary acne, the use of Metrogyl gel should be combined with oral antibiotics.
When applied to a large surface area of the skin or in case of prolonged use of Metrogyl gel, there is a possibility of developing systemic side effects.
The drug should be prescribed with caution to patients with impaired hematopoietic function.
Metronidazole for topical use is not effective for the treatment of telangiectasia, which occurs with erythematosus.
Propyl parahydroxybenzoate (E216) and methyl parahydroxybenzoate (E218), which are part of the drug, can cause an allergic reaction (possibly delayed).
Use during pregnancy and lactation.
When taken orally, metronidazole crosses the placental barrier into breast milk in very significant concentrations.
Despite the fact that when applied topically, the concentration of metronidazole in the blood is low, Metrogyl gel is contraindicated in the first trimester of pregnancy, and in the second and third trimester it can be used if absolutely necessary.
Breastfeeding should be stopped during treatment.
Children. Do not use in children.
The ability to influence reaction speed when driving vehicles or operating machinery. The use of the drug at the indicated dose does not affect driving or working with potentially dangerous mechanisms.
Metrogyl solution for infusion 500 mg bottle 100 ml 1 pc. in Barnaul
Pharmacological action: Pharmacodynamics
Blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (to a greater extent into vascular smooth muscle cells than into cardiomyocytes).
The antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles:
— for angina pectoris, reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces peripheral vascular resistance, reduces afterload on the heart, and reduces myocardial oxygen demand;
- expanding the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents spasm of the coronary arteries (including those caused by smoking).
In patients with stable angina, a single daily dose increases exercise tolerance, slows down the development of angina attacks and ischemic depression of the ST segment, reduces the frequency of angina attacks and the consumption of nitroglycerin and other nitrates.
It has a long-term dose-dependent effect. The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over 24 hours (with the patient lying and standing).
Orthostatic hypotension with amlodipine is quite rare. Amlodipine does not cause a decrease in exercise tolerance or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy. It does not affect myocardial contractility and conductivity, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not have any adverse effect on metabolism and plasma lipid concentrations and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout. A significant decrease in blood pressure is observed after 6–10 hours, the duration of the effect is 24 hours.
In patients with cardiovascular diseases (including coronary atherosclerosis with damage to one vessel and up to stenosis of 3 or more arteries, atherosclerosis of the carotid arteries), who have had myocardial infarction, percutaneous transluminal coronary angioplasty (PTCA), or in patients with angina, the use of amlodipine prevents the development of intimal thickening - media of the carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, coronary artery bypass grafting; leads to a decrease in the number of hospitalizations for unstable angina and progression of CHF; reduces the frequency of interventions aimed at restoring coronary blood flow.
Does not increase the risk of complications and deaths in patients with CHF (III–IV functional class according to the NYHA
) during therapy with digoxin, diuretics and ACE inhibitors.
In patients with CHF (III–IV functional class according to the NYHA
) of non-ischemic etiology, when using amlodipine, there is a risk of pulmonary edema.
Pharmacokinetics
After oral administration, amlodipine is well absorbed from the gastrointestinal tract. Average absolute bioavailability is 64–80%, Cmax in blood serum is determined after 6–12 hours. Css are achieved after 7–8 days of therapy.
Concomitant food intake does not affect the absorption of amlodipine. The average Vd is 21 l/kg, which indicates that most of the drug is in the tissues, and the smaller part is in the blood. Most of the drugs in the blood (97.5%) bind to blood plasma proteins. Amlodipine undergoes slow but active metabolism in the liver with no significant first-pass effect through the liver. Metabolites do not have significant pharmacological activity.
After a single dose, T1/2 varies from 35 to 50 hours; with repeated administration, T1/2 is approximately 45 hours. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% unchanged, and 20–25% - through the intestines with bile. The total clearance of amlodipine is 0.116 ml/s/kg (7 ml/min/kg; 0.42 l/h/kg).
Elderly patients.
In elderly patients (over 65 years of age), compared to young patients, the elimination of amlodipine is slower (T1/2 - 65 hours), but this difference is not clinically significant.
Liver failure.
Prolongation of T1/2 in patients with liver failure suggests that with long-term administration, the accumulation of drugs in the body will be higher (T1/2 - up to 60 hours).
Kidney failure.
Renal failure does not significantly affect the kinetics of amlodipine. Amlodipine penetrates the BBB. It is not removed by hemodialysis.
Interactions
When applied topically in recommended doses, no systemic interaction of Metrogyl gel with other drugs was detected. however, caution should be exercised when prescribing Metrogyl gel with certain medications.
Warfarin and other coumarin anticoagulants. Metronidazole enhances the anticoagulant effect, which leads to an increase in the time of prothrombin formation.
Phenobarbital. When used simultaneously with metronidazole, the antimicrobial activity of the latter decreases. The reason is the accelerated metabolism of metronidazole.
Disulfiram. Concomitant use increases the toxicity of the drugs, which can lead to the development of neurological symptoms.
Cimetidine. Suppresses the metabolism of metronidazole, which may lead to increased concentrations of metronidazole in the blood serum.
During systemic therapy with metronidazole, it is necessary to refrain from drinking alcohol, since a disulfiram-like reaction is possible.
Metrogyl for rosacea
Rosacea is a fairly common disease that requires complex treatment and intervention for results.
The disease often goes unnoticed until health consequences appear, which is why it is worth noticing at the first symptoms. If, after visiting a cosmetologist, a diagnosis of Rosacea is made, it is necessary to begin comprehensive treatment. Metrogyl, many cosmetologists recommend using it in addition to the main prescribed treatment to obtain a more pronounced result.
It is worth taking a closer look at the treatment and the necessary comprehensive measures that cannot be excluded from daily care.
Note!
The description of the drug Metrogyl gel tube 30g on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Is it worth using Metrogyl gel?
If you survey those who have already used Metrogyl acne gel, the reviews will contain the following advantages:
- pronounced anti-inflammatory effect;
- improvement of the general condition of the skin;
- fewer rashes already in the first month of use;
- rapid healing of wounds and abrasions.
If there are no visible improvements within three weeks, contact your dermatologist; you may need to use additional products to enhance the effect of the gel or choose a different drug.
The result of treatment depends on many factors: the causes of the rash, the severity of the disease, the individual characteristics of the body and compliance with the rules of use.
Normalization of the daily routine
Insufficient sleep or drinking clean water can also negatively affect the skin, causing obvious problems in the form of inflammatory processes. Insufficient sleep affects the body directly, especially if the lack continues for a long time. If you have problems with your skin condition, look at your napkin and the amount of clean water.
As for water, most of a person consists of it, and therefore it is necessary to drink liquid for normal well-being and the functioning of internal organs. It is important to drink clean water, not carbonated water or juices or teas. Water without gases and various chemical additives is best absorbed, which is why it is better to drink pure liquid directly.
The amount of clean water is calculated individually for a person, depending on his body weight, the characteristics of the excretory system, the presence of diseases, etc.
Controlling the amount of vitamins
A common cause of rosacea is an insufficient amount of vitamins, which causes problems with the condition of the skin, hair, and nails. As the problem appears, it is recommended to take a blood test for vitamins and their amounts.
Rosacea is a common disease that requires complex treatment and impact on the result. The disease often goes unnoticed until health consequences occur, so it is worth treating it at the first symptoms.
If, after visiting a cosmetologist, a diagnosis of rosacea is made, it is necessary to begin comprehensive treatment. Many cosmetologists recommend using Metrogyl in addition to the main prescribed treatment to achieve a more pronounced result.
If the examination results show an insufficient amount of essential vitamins and microelements, you will need to take them in medicinal form. At the same time, the treatment also remains complex, that is, it will be necessary to influence the inflammatory processes to obtain results.
UV protection
Excessive exposure of the skin surface to sunlight negatively affects its condition, and is also the cause of the active development of rosacea. Therefore, when you are in the sun, you need to wear sunscreen and glasses.
If a person has already been directly diagnosed with rosacea, it is recommended to limit exposure to sunny areas and use UV protection methods when leaving the room. Otherwise, the disease will progress, which will require additional measures.
Correct use of decorative cosmetics
Often the development and course of rosacea is influenced by the use (for women in particular) of excessive amounts of decorative cosmetics. The purpose of use is to achieve a matte effect, that is, the absence of shine on the face, neck, and décolleté area.
To avoid the negative development of the disease, look at the composition of the cosmetic product that is directly purchased. The products should not contain potential skin irritants, as the course of the disease can significantly worsen. If cosmetic products do not contain aggressive agents (such as alcohol or acids), it will be possible to maintain the normal acid-base balance of the skin.
All products that are directly applied to the surface of the skin must be hypoallergenic, since there is a risk of aggravating the situation due to the occurrence of an allergic reaction to certain components.
The solution is to purchase cosmetics that have an anti-inflammatory effect and also allow for constant use without side effects.
It is worth switching to completely natural cosmetics that do not contain vitamins A and D. If you have a diagnosis of rosacea, the use of mineral cosmetics is quite easy to tolerate.
It is recommended that before selecting a cosmetic bag, as well as before directly purchasing caring creams, visit a cosmetologist who will determine your skin type and conduct a consultation on how to combat the disease. Expert advice will speed up skin restoration and help achieve bright results without long-term medication. There is a possibility that you will also have to visit a doctor and undergo a series of tests. The appearance of inflammatory processes is a consequence of disturbances in the functioning of internal organs or an increase in hormones.
The use of moisturizing creams and similar products is mandatory when treating rosacea, as they relieve the symptoms of the disease. Regular application of a moisturizer suitable for your skin type can significantly reduce itching, unpleasant tingling, and prevent burning and tightness of the skin. It is important to find a good cream, as there is a risk of exacerbation of the situation and the appearance of new unpleasant symptoms of the disease.
Only a full examination, comprehensive treatment, and the use of high-quality medications can give a fairly positive effect.
