Antikva Rapid - instructions for use, dose, side effects, contraindications

Active substance:	Dosage	Dosage
	60 μg	120 μg
Desmopressin acetate	0.0675 mg	0.1350 mg
(in terms of desmopressin)	0.060 mg	0.120 mg
Excipients:
Sodium fumarate	2.0000 mg	2.0000 mg
Mannitol	92.9325 mg	92.8650 mg
Croscarmellose sodium	5,0000 mg	5,0000 mg

Description:

Dosage of 60 mcg: Round biconvex tablets white or almost white.

Dosage of 120 mcg: Round biconvex tablets white or almost white.

Pharmacotherapeutic group:Vasopressin and its analogues

ATX: & nbsp

H.01.B.A.02 Desmopressin

Pharmacodynamics:The antiqua Rapid preparation contains desmopressin - structural analogue of the natural hormone arginine-vasopressin, obtained as a result of changes in the structure of the molecule of vasopressin. These structural changes lead, in combination with a significantly enhanced antidiuretic ability, to a less pronounced effect on the smooth musculature of the vessels and internal organs compared with vasopressin, which leads to the absence of undesirable spastic side effects. In contrast, vasopressin acts longer and does not cause an increase in blood pressure (BP). The drug increases the permeability of the epithelium of the distal convoluted tubules of the nephron for water and increases its reabsorption. Application of the drug Rapid antiquity with central diabetes insipidus leads to a decrease in the volume of urine output and one temporary increase of osmolarity of urine and decrease of osmolarity of blood plasma. This leads to a decrease in the frequency of urination and a decrease in nocturnal polyuria.

Pharmacokinetics:

Bioavailability of desmopressin in sublingual form at doses of 200, 400 and 800 μg is about 0.25%.

The maximum concentration (C_m_Oh) desmopressin in blood plasma is achieved within 0.5-2 hours after taking the drug and is directly proportional to the value of the dose: after taking 200, 400 and 800 mcg C_m_Oh was 14 pg / ml, 30 pg / ml, and 65 pg / ml, respectively.

Desmopressin does not penetrate the blood-brain barrier.

Desmopressin is excreted by the kidneys, the elimination half-life is 2.8 hours.

Indications:

- Non-diabetes mellitus of central origin;

- Polyuria / polydipsia after hypophysectomy or operations in the area of the "Turkish saddle";

- Primary nocturnal enuresis in adults and children older than 5 years;

- Nocturia in adults associated with nocturnal polyuria (increased urination at night, exceeding the capacity of the bladder and causing the need to get up at night more than once to empty the bladder) - as a symptomatic therapy.

Contraindications:

- Hypersensitivity to desmopressin or any auxiliary substance of the drug;

- Habitual or psychogenic polydipsia (with a urine volume of 40 ml / kg / 24 hours);

- Diagnosed or suspected chronic heart failure and other conditions requiring the appointment of diuretics;

- Hyponatremia, including in the anamnesis;

- Renal failure of moderate to severe severity (creatinine clearance (CK) less than 50 ml / min);

- Syndrome of inadequate production of antidiuretic hormone;

- Children under 5 years;

- Age 65 years and older - when used for symptomatic therapy of nocturia;

- Polydipsia in chronic alcoholism.

Carefully:

Chronic renal failure (QC more than 50 ml / min), fibrosis of the bladder, cystic fibrosis, ischemic heart disease, arterial hypertension, disturbance of water electrolyte balance, potential risk of increased intracranial pressure, risk of thrombosis, during pregnancy, incl. at a pre-eclampsia, elderly age (65 years and is more senior) at application for treatment of a diabetes insipidus.

Pregnancy and lactation:

Pregnancy

Limited data on the use of desmopressin in pregnant women with diabetes insipidus (N=53) evidence that desmopressin does not adversely affect the course of pregnancy or the health of a pregnant, fetus or newborn. Studies in animals have not revealed a direct or indirect adverse effect on the course of pregnancy, embryonic or intrauterine development, childbirth or postpartum development.

Pregnant women desmopressin should be appointed only after a thorough assessment of the benefits and risks. The drug is prescribed only when the expected benefit for the mother exceeds the potential risk to the fetus. Use the drug in pregnant women with caution, it is recommended that regular monitoring of blood pressure.

Breastfeeding period

Study of breast milk of women who received desmopressin in a dose of 300 μg intranasal, showed that the amount of desmopressin that can enter the baby's body is too small and can not affect its diuresis.

Dosing and Administration:

Inside, keep in your mouth until completely dissolved. Tablets, dispersible in the oral cavity, should not be taken with wet hands, as the tablet can begin to dissolve. DO NOT PREPARE THE TABLET LIQUID! The optimal dose of Antiqua Rapid is selected individually. The dosage ratios between oral tablets and tablets dispersible in the oral cavity are given in the table:

Pills	Tablets, dispersible in the oral cavity
0.1 mg	60 μg
0.2 mg	120 μg

Preparation Antiqua Rapid must be taken after some time after eating, as eating reduces the absorption of the drug and its effectiveness

Non-diabetes mellitus of central genesis and polyuria / polydipsia after hypophysectomy or operations in the field of "Turkish saddle"

At the beginning of treatment, the optimal dose of the drug is determined by the doctor individually, taking into account the osmolality and volume of urine. During the therapy it is necessary to control the duration of sleep and the water-electrolyte balance.

The recommended initial dose of the drug is Antikva Rapid 60 μg 3 times a day. In the subsequent dose change depending on the onset of therapeutic effect. The recommended daily dose is in the range of 120-720 μg. The optimal maintenance dose is 60-120 μg 3 times a day.

If there are signs of fluid retention / hyponatremia, discontinue therapy and adjust the dose of the drug.

Primary night enuresis

The optimal therapeutic dose is determined individually and adjusted according to the patient's response to treatment.

The recommended initial dose is 120 mcg per night. In the absence of effect, the dose may be increased to 240 μg. During treatment, it is necessary to limit fluid intake in the evening.

If there are signs of fluid retention / hyponatremia, discontinue therapy and adjust the dose of the drug.

The recommended course of continuous treatment is 3 months. The decision to continue treatment is made on the basis of clinical data, which will be observed after the drug is discontinued within 1 week.

Nocturia

The recommended initial dose is 60 mcg at night. If there is no effect within 1 week, increase to 120 mcg and then to 240 mcg when the dose is increased at a frequency of no more than 1 time per week.

If after 4 weeks of treatment and dose correction adequate clinical effect is not observed, continue taking the drug is not recommended.

It is necessary to monitor compliance with the restriction of fluid intake.

Special patient groups

Elderly patients

Contraindicated use of the drug at the age of 65 years and older for symptomatic therapy of nocturia. In patients aged 65 years and over, use the drug to treat diabetes insipidus with caution. When prescribing desmopressin to elderly patients, it is necessary to monitor the sodium content in the blood plasma before the start of treatment, 3 days after the start of treatment or with an increase in the dose,and also if necessary during the administration of the drug.

Side effects:

The use of the drug without concomitant restriction of fluid intake may lead to fluid retention and / or hyponatremia, which may be asymptomatic or accompanied by the following symptoms: headache, nausea and / or vomiting, weight gain; in severe cases, convulsions, which are combined with a violation of consciousness until a prolonged loss of consciousness. These symptoms are especially characteristic for children or the elderly, depending on their general condition.

Frequency of side effects: very often (≥ 1/10), often (≥ 1/100 to <1/10), infrequently (≥ 1/1000 to <1/100), rarely (≥ 1/10000 to <1/1000 ), very rarely (<1/10000), the frequency is not established (at present, there are no data on the prevalence of adverse reactions, they were detected during the postemergence application of desmopressin).

When used in adults:

The table lists the adverse reactions and the frequency of their occurrence, based on data from a clinical trial in patients with nocturia (N=1557) and with the post-marketing application of the drug for all indications for use (including with diabetes insipidus).

System-Organ Class	Highly often	Often	Infrequently	Rarely	Frequency not set
Immune system disorders					Anaphylactic reactions
Disorders from the metabolism and nutrition		Hyponatremia			Dehydration , hypernatremia
Disorders of the psyche			Insomnia	Confusion of consciousness
Disturbances from the nervous system	Headache	Dizziness	Drowsiness, paresthesia		Convulsions, asthenia *, coma
Disturbances on the part of the organ of sight			Decreased visual acuity
Hearing disorders and labyrinthine disorders			Vertigo
Heart Disease			Heart palpitations
Vascular disorders		Arterial hypertension	Orthostatic hypotension
Disturbances from the respiratory system, chest and mediastinal organs			Dyspnea
Disorders from the gastrointestinal tract		Nausea, vomiting, abdominal pain, diarrhea, constipation	Dyspepsia, flatulence, bloating
Disturbances from the skin and subcutaneous tissues			Increased sweating, itching, skin rash, urticaria	Allergic dermatitis
Disturbances from musculoskeletal and connective tissue			Muscle spasms, myalgia
Disorders from the kidneys and urinary tract		Dysfunction of urinary bladder, urinary disruption
General disorders and disorders at the site of administration		Peripheral edema, fatigue	Feeling of discomfort, chest pain, flu-like syndrome
Laboratory and instrumental data			An increase in body weight, an increase in the activity of liver enzymes, hypokalemia

* Unwanted reactions were observed only in patients with diabetes insipidus.

When used in children:

The table lists the adverse reactions and the frequency of their occurrence based on data from the clinical trial (N=1923) and with the post-marketing application of the drug for the treatment of primary nocturnal enuresis in children.

System-Organ Class	Highly often	Often	Infrequently	Rarely	Frequency not set
Immune system disorders					Anaphylactic reactions
Disorders from the metabolism and nutrition					Hyponatremia
Disorders of the psyche			Emotional lability, the manifestation of aggression	Anxiety, nightmares, a sharp change of mood	Behavior change, emotional disorders, depression, hallucinations, insomnia
Disturbances from the nervous system		Headache		Drowsiness	Violation of attention, psychomotor hyperactivity, convulsions
Vascular disorders				Arterial hypertension
Disturbances from the respiratory system, chest and mediastinal organs					Nose bleed
Disorders from the gastrointestinal tract			Nausea, vomiting, diarrhea, pain in the stomach
Disturbances from the skin and subcutaneous tissues					Allergic dermatitis, skin rash, increased sweating, urticaria
Disorders from the kidneys and urinary tract			Dysfunction of urinary bladder, urinary disruption
General disorders and disorders at the site of administration			Peripheral edema, fatigue	Irritability

Attention! Desmopressin may have an antidiuretic effect. Administration of the drug Antiqua Rapid, tablets dispersible in the oral cavity, without simultaneous restriction of fluid intake, can lead to fluid retention in the body, accompanied by hyponatremia, manifested by headache, abdominal pain, nausea, vomiting, weight gain, dizziness, confusion, malaise and, in severe cases, can lead to convulsions, swelling of the brain and coma.In particular, the highest risk for the development of the above complications in children under the age of 1 year, or in elderly patients (over 65 years), depending on the general state of health.

In the treatment of nocturia in adults, hyponatremia often develops at the beginning of the drug intake or with an increase in the dose. Hyponatremia is reversible. When taking the drug Rapid antiquity, it is necessary to control the water-electrolyte balance.

In the treatment of possible hypertension due to fluid retention. Patients with ischemic heart disease may develop angina pectoris.

If any of the unwanted reactions listed in the manual is aggravated, or if you notice any other undesirable reactions not listed in the instructions, inform the doctor about it.

Overdose:

Overdose Symptoms

Symptoms of overdose may occur if desmopressin is used at too high a dose or if the fluid is consumed excessively at the same time or shortly after taking desmopressin.

Symptoms of overdose: weight gain due to fluid retention, headache, nausea, in severe cases - hyperhydration (water intoxication), accompanied by convulsions, confusion or loss of consciousness.

Overdose can be observed in children at an early age due to insufficiently careful selection of a dose.

Treatment. In case of an overdose, depending on the degree of its severity, you should reduce the dose of the drug, increase the time between taking the drug during the day or stop taking the drug. If you suspect a brain swelling, you need immediate admission to the intensive care unit. When cramps occur, immediate intensive care is required. The specific antidote of desmopressin is not known. For the induction of diuresis, it is possible to use diuretics, such as furosemide, with the simultaneous control of the content of electrolytes in blood plasma.

Interaction:

Tricyclic antidepressants, selective serotonin reuptake inhibitors, chlorpromazine, chlorpropamide, carbamazepine and other drugs that can cause the syndrome of inadequate secretion of antidiuretic hormone, can enhance the antidiuretic effect of desmopressin and increase the risk of fluid retention and hyponatremia.

Indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDs) when combined with desmopressin can induce fluid retention and hyponatraemia.

The combination with loperamide can lead to a threefold increase in the concentration of desmopressin in plasma and increase the risk of side effects (fluid retention, hyponatremia). There is a possibility that other drugs that lower tone and motor smooth bowel muscles may have a similar effect.

With simultaneous use with oxytocin, one should take into account the intensification of the antidiuretic effect and the decrease in uterine perfusion.

Clofibrate can enhance the antidiuretic effect of desmopressin. With the simultaneous use of the preparation of Antiqua Rapid with the above preparations for the prevention of hyponatremia, a regular determination of the concentration of sodium in the blood plasma is necessary.

The intake of glibenclamide and lithium preparations can reduce the antidiuretic effect of desmopressin.

Interaction with drugs metabolized in the liver is unlikely, because desmopressin has no significant effect on hepatic metabolism according to the results of a liver microsome in vitro. Research in vivo not conducted.

Special instructions:

It is mandatory to limit to a minimum the intake of fluid 1 hour before admission and within 8 hours after taking the drug in patients with primary nocturnal enuresis and nocturia. Failure to adhere to the rules of taking the drug may cause fluid retention in the body and / or hyponatremia, which can be manifested by the following symptoms: headache, dizziness, nausea, vomiting, weight gain, in severe cases - cerebral edema, convulsions and coma. The safety of the drug during long-term admission in cases of nocturnal enuresis has not been investigated. Patients should be carefully instructed about the need to comply with the regime of fluid intake. It is necessary to warn the patient about the need to avoid overloading with liquid and stop taking desmopressin against the background of vomiting and diarrhea, until the water balance is restored. Before starting treatment, make sure the patient agrees to limit fluid intake.

The risk of hyponatremic convulsions caused by hyponatremia can be minimized if the recommended initial dose of desmopressin is used and the concomitant use of drugs that increase the secretion of antidiuretic hormone is avoided.

For the diagnosis of nocturnal polyuria in patients with nicture 2 days before the start of treatment, it is necessary to monitor the frequency and volume of urination. The increase in urination at night, exceeding the capacity of the bladder or exceeding 1/3 of the daily volume of urine, is considered as nocturnal polyuria.

When receiving desmopressin for the treatment of nocturnal enuresis, there were cases of cerebral edema and seizures in healthy children and adolescents. Based on the available information, it can be concluded that the risk of developing cerebral edema and seizures is greatest in the first week of taking the drug.

Most often, hyponatremia occurs in elderly patients (over 65 years) with diabetes insipidus with an initially low concentration of sodium in the blood plasma and polyuria 2,8-3 liters per day. Preparation Antiqua Rapid used them with extreme caution. When using the drug in these cases, it is necessary to determine the concentration of sodium in the blood plasma before the start of the drug, 3 days after the start of the dose and at each dose increase. It is necessary to monitor the patient's condition during the entire period of taking the drug Rapid Antique.

Antikva preparation Rapid should be used with caution in patients with chronic renal failure, fibrosis of the bladder, cystic fibrosis, coronary heart disease, hypertension, with a potential risk of increased intracranial pressure; violation of water-electrolyte balance; patients with risk of thrombosis; in pregnancy, including pre-eclampsia; in elderly patients (over 65 years of age) when used to treat diabetes insipidus. In patients with hypertension or chronic kidney disease, the symptoms described in the section "Side effect" may develop. Particular care should be taken with the use of the drug Rapid antidepressant in children and elderly patients, or patients at risk of increasing intracranial pressure, trying to prevent fluid retention in the body.

Patients and, when using the drug in children, their parents should be informed about the need to limit fluid intake and stopping desmopressin in case of headache and / or nausea, vomiting, systemic infectious diseases and fever, and do not resume until normal water levels Electrolyte balance.

To reduce the risk of developing hyponatremia or fluid retention, it is necessary to reduce fluid intake in the following cases:

1 when taking medications that lead to the syndrome of inadequate production of antidiuristic hormone (tricyclic antidepressants, selective serotonin reuptake inhibitors, chlorpromazine, chlorpropamide and carbazepine);

2 with the concomitant use of NSAIDs.

In the course of treatment, weight changes should be monitored.

The use of the drug in elderly patients (65 years of age and starting) for symptomatic therapy with nocturia is contraindicated.

One should assess the presence of bladder dysfunction and urethral obstruction before starting treatment. In cases of acute incontinence, dysuria and / or nocturia, urinary tract infection, with a suspected bladder or prostate tumor, with polydipsia and decompensated diabetes mellitus, it is necessary to diagnose and treat these conditions and diseases before starting treatment with Antiqua Rapid .

Before the beginning of treatment it is necessary to conduct therapy for insufficiency of the function of the adrenal cortex or thyroid gland.

Effect on the ability to drive transp. cf. and fur:

Currently, there is no data on the possible effect of the Antiqua Rapid drug on the ability to drive vehicles and work with mechanisms. Nevertheless, the use of the drug may lead to the development of side effects such as dizziness, headache, which can adversely affect the ability to drive vehicles and carry out potentially dangerous activities that require increased concentration and speed of psychomotor reactions. It is recommended to use caution when driving vehicles or working with machinery.

Form release / dosage:

Tablets dispersible in the oral cavity, 60 mcg and 120 mcg.

Packaging:

For 30 or 100 tablets in a bottle of high-density polyethylene, closed with a polypropylene lid (with a dehumidifier and protection from accidental opening by children).

Or 10 tablets in a planar cell packaging made of polyamide / aluminum / PVC composite material or from PVC / PVDC film and aluminum foil foil. Each vial or 1, 3 or 10 contour squares, together with the instructions for use, are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004562

Date of registration:28.11.2017

Expiration Date:28.11.2022

The owner of the registration certificate:FARMSTANDART-UFAVITA, JSC FARMSTANDART-UFAVITA, JSC Russia

Manufacturer: & nbsp

FARMSTANDART-UFAVITA, JSC Russia

Information update date: & nbsp10.01.2018

Illustrated instructions

Instructions

Antique Rapid (Antique Rapid)