No-shpa: instructions for use,contraindications, side effects, indications, dosage

Update: October 2018

No-SPA (NO-SPA) – a popular drug that provides fast
antispasmodic effect on smooth muscle.
It is applied for:

  • etiotropic therapy to eliminate muscle spasm,
    serving as the basis of the pathological condition;
  • symptomatic treatment of smooth muscle spasm which is
    a symptom of the disease, without affecting its pathogenesis;
  • premedication during the preparation of patients to some
    procedures (catheterization of ureters, urethra
    etc.).

Since the drug acts solely on smooth muscles, its
practice in situations where there are contraindications to
antispasmodics from the group of anticholinergic blockers (hypertrophy
prostate, glaucoma).

Pharmacological group: myotropic antispasmodic.

Drotaverinum or No-shpa

Surely each of us had to take the famous yellow
tablets with a special finish for those or other problems with
health The composition of the drug is the active substance.
Drotaverine, and it is under this name that the most
popular competitor No-shpy and similar in composition. What’s the difference
between Drotaverinum and No-spoy?

Having studied the instructions for the drugs, it becomes clear that the composition and
principle of action, and the effect is similar. therefore
a reasonable question arises – is there any sense to overpay for no-shpu?
No-shpa is an original drug patented drug
the form. Having a patent is not only an excuse for high costs.
drug, but also certain obligations that are imposed
on the manufacturer: the quality of raw materials, production control,
The safety of the drug must be top notch. For,
to obtain a patent, the drug must comply with a number of strict
requirements and undergo the necessary clinical trials.

Drotaverine is a generic drug offered to consumers under
international, which means unpatented name. Clinical
The effectiveness of generics is not fully proven because
this group of drugs are put forward less stringent
requirements.

It turns out that the patented drug is exposed to more
the number of tests before getting to the pharmacy counter. but
This does not mean that the generic negatively affects
health.

Physical and chemical properties, composition, price

The drug is available in two dosage forms – tablets for
internal reception and solution for the / m and / in the introduction.

Main substance Excipients Physicochemical properties

No-shpa pills

On 6, 20, 24 tablets in aluminum blisters. 60, 100
tablets in polypropylene bottles, in packs from a cardboard.

  • Number 6: 50-70 rubles;
  • № 24: 180-220 rubles.

Drotaverine Hydrochloride: 40 mg

Magnesium stearate 3 mg, corn starch 35 mg, talc 4 mg,
Povidone 6 mg, lactose monohydrate 52 mg.
Yellowish-greenish round biconvex tablets,
having a “spa” engraving on one side.

Solution

On 2 ml in glass ampoules from dark glass with a notch
rift. On 5 ampoules in packing, in packs cardboard.

  • Number 25: 450-480 rubles.

Drotaverine hydrochloride: 20 mg in 1 ml or 40 mg in 1 ampoule

Sodium disulfite 2 mg, 96% ethanol – 132 mg, water d / and – to
volume of 2 ml.
Transparent greenish yellow solution.

pharmachologic effect

Drotaverine hydrochloride is an isoquinoline derivative with potent
antispasmodic effect on smooth muscle. This effect
possible by inhibiting an enzyme called PDE
(phosphodiesterase).

PDE is involved in the hydrolysis reaction of cAMP to AMP. Inhibition
phosphodiesterase is characterized by an increase in the concentration of cAMP,
triggering a chain reaction. cAMP in high concentrations is
activator of cAMP-dependent phosphorylation of MLCK (lung kinase
chains of myosin). This leads to a decrease in the affinity of MLCK to
Ca2 + -calmodulin complex, and inactivated form KLCM
creates muscle relaxation.

cAMP affects the cytosolic concentration of the Ca2 + ion, lowering it.
This is due to the stimulation of Ca2 + transport to the sarcoplasmic
reticulum and extracellular space.

The effectiveness of drotaverine hydrochloride depends on the concentration
phosphodiesterase enzyme in tissues, which is significantly
varies.

Hydrolysis of cAMP in the muscle tissue of the heart and smooth muscles
vessels is performed using PDE3 isoenzyme. This explains
no serious adverse reactions from the CCC
antispasmodic activity.

Selective PDE4 inhibitors, which is Drotaverine, can
reduce the sensitivity of the uterus to the action of the hormone oxytocin and
lead to accelerated relaxation of the muscular tissue of the body that
allows you to stop preterm labor.

In addition to the antispasmodic effect, drotaverine reduces swelling and
muscle inflammation. Elimination of spasm leads to improvement
blood supply to organs. The drug is effective for pain as well
helps to restore the passage of the inner contents of the hollow
organs.

However, drotaverine is not directly intervenes in the mechanism
pain sensitivity and does not erase the symptoms of acute conditions
unlike analgesics.

The effectiveness of Drotaverinum is high in smooth muscle spasms.
tissues of neurogenic and muscular origin. No-spa relaxes
smooth muscle fibers of the digestive tract, urinary and biliary
ways.

Pharmacokinetics

After ingestion, the active substance is fully and quickly.
absorbed, evenly distributed through the tissues and penetrates into
smooth muscle cells. About 65% of the active blood enters
substances. The maximum concentration in the blood is determined by
45-60 minutes after administration. Slightly passes through the placental
barrier. Does not enter the central nervous system and does not affect the autonomic nervous system
the system.

When i / v or i / m administration, drotaverine binds to plasma
proteins 95-98% with the maximum effect in 30
minutes

The metabolism of the substance occurs to the liver cells through reactions
O-deethylation. Drotaverine metabolites conjugate to
glucuronic acid.

Excreted by the kidneys (more than 50%) and intestines (30%) in the form
metabolites, complete elimination occurs within 72 hours.

Indications for use

The instructions for use shpy are the following indications
for etiotropic therapy:

  • Spasms of smooth muscle tissue in diseases of the biliary tract
    ways: cholangiolithiasis, cholecystolithiasis, pericholecystitis, cholecystitis,
    cholangitis, papillitis;
  • Spasms of smooth muscle tissue in urinary pathologies
    systems: nephrolithiasis, pyelitis, urethrolithiasis, cystitis, spasms and
    tenesmus of the bladder;

What else helps No-shpa? As a drug auxiliary
therapy (tablets or solution when it is impossible to take
tablets):

  • with spasms of smooth muscle tissue of the gastrointestinal tract: gastritis, YABZH and
    Duodenal ulcer, pyloric spasms and cardia of the stomach, colitis,
    spastic colitis with constipation, enteritis, dysfunction of the sphincter of Oddi,
    irritable bowel syndrome;
  • with tension headaches (pill form). No-shpa
    not effective against headaches associated with migraine or increased
    ICP;
  • with dysmenorrhea.

Contraindications

  • severe renal or heart failure;
  • children’s age up to 6 years (tablets). Nosh-pa children in the form of
    the solution is not appointed until 18 years;
  • lactation period (due to the lack of clinical data on
    penetration of the drug into the mother’s milk);
  • hereditary intolerance to galactose monosaccharide syndrome
    glucose-galactose malabsorption, lactase deficiency (for
    tablets);
  • hypersensitivity to sodium disulfite (for solution).

special instructions

With caution, the drug is prescribed for arterial hypotension,
since there is a risk of collapse during pregnancy and
pediatrics When the / in the introduction of people with low blood pressure should
to be in a supine position.

There may be complaints of dysfunction of the gastrointestinal tract when using the drug in
people with lactose intolerance (52 mg of lactose per 1 tablet).

Tablet form does not affect the ability to perform work,
requiring significant concentration of attention, and driving cars.
After parenteral administration, no-shpa should refrain from
accurate work and driving cars.

No-shpa при беременности

Very often, the drug is prescribed in early pregnancy.
with uterus tone to reduce the risk of spontaneous
miscarriage.

Animal studies and retrospective data on
clinical use of drotaverine in pregnant women
indicate that the drug in therapeutic dosages is not
had neither embryotoxic nor teratogenic effects on the fetus.
But, since the drug to some extent penetrates
placenta, the appointment is justified in the presence of real risk
miscarriage.

The drug can not be used in the period of labor,
since there is a risk of atonic bleeding in
postpartum period.

Dosage no-shpy

The duration of treatment is individual. On their own
It is allowed to take the drug for 1-3 days.

For pills

  • Adult patients: 120-240 mg per day, dividing the dose by 2-3
    reception. The maximum dose for a single dose – 80 mg.
  • Дети 6-12 лет: 80 мг в сут, разделив на 2 reception.
  • Дети старше 12 лет: 160 мг в сут, разделив на 2-4 reception.

For maximum effectiveness, the drug is taken after 1 hour.
after eating, drinking plenty of water.

For solution

Adult patients: 40-240 mg per day, divided into 1-3 injections.
In acute spasmodic pains, the drug is administered in / in slowly, with a dose of
40-80 mg for 30 seconds. V / m injections are entered without dilution
solution by other drugs.

The patient can usually assess the effectiveness of the drug.
observing a significant decrease or disappearance of pain
spasmodic syndrome for several hours after ingestion
pills or injections.

Side effects

  • CCC: rarely observed tachycardia or a decrease in blood pressure;
  • Nervous system: insomnia, headache and
    dizziness;
  • Gastrointestinal: nausea and constipation sometimes observed;
  • The immune system: rarely develop allergic reactions
    (rash, itching). There have been cases of anaphylactic shock with a fatal
    outcome and without such (frequency unknown). In persons with bronchial
    asthma or allergies may develop bronchospasm when applied
    solution of the drug.
  • Local reactions: swelling at the injection site.

Overdose

With a significant excess of therapeutic dose develops
violation of cardiac conduction and rhythm up to complete blockade
bundle branch block and cardiac arrest. Treatment only
stationary.

Drug interactions

  • Levodopa – weakening of antiparkinsonian action, strengthening
    rigidity and tremor;
  • Other antispasmodics – increased antispasmodic action;
  • Tricyclic antidepressants – arterial enhancement
    hypotension (only when combined with the solution of No-shpy);
  • Morphine – a decrease in spasmogenic activity (only with
    combination with solution No-shpy);
  • Phenobarbital – increased spasmolytic effect of No-shpy;
  • Drugs binding to plasma proteins – possibly
    occurrence of pharmacodynamic and toxic effects of data
    drugs.

Analogs

No-shpa форте, Дротаверин, Дротаверин-Форте, Spazmonet,
Drotaverin-STI, Spasmol.

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  • Drotaverine Hydrochloride

40 mg. 20 tab. 12-20 rub.

  • Spazmonet

40 mg. 20 tab. 55-80 rub.

  •  Drotaverin Forte

80 mg. 20 tab. 50 rub.

  • Spasmol

40 mg. 20 tab. 32 руб.

Автор: врач-гигиенист, эпидемиолог

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