Spekzo Tx Tube

Spekzo Tx Tube Uses, Dosage, Side Effects, Food Interaction and all others data.

Extracted from the dried leaves of bearberry plant in the genus Arctostaphylos and other plants commonly in the Ericaceae family, arbutin is a beta-D-glucopyranoside of Hydroquinone. It is found in foods, over-the-counter drugs, and herbal dietary supplements . Most commonly, it is an active ingredient in skincare and cosmetic products as a skin-lightening agent for the prevention of melanin formation in various skin conditions that involve cutaneous hyperpigmentation or hyperactive melanocyte function . It has also been used as an anti-infective for the urinary system as well as a diuretic . Arbutin is available in both natural and synthetic forms; it can be synthesized from acetobromglucose and Hydroquinone . Arbutin is a competitive inhibitor of tyrosinase (E.C.1.14.18.1) in melanocytes , and the inhibition of melanin synthesis at non-toxic concentrations was observed in vitro. Arbutin was shown to be less cytotoxic to melanocytes in culture compared to Hydroquinone .

At non-toxic concentrations, arbutin inhibited the activity of tyrosinase in cultured human keratinocytes, while having minimal effect on the expression of tyrosinase mRNA or the synthesis of the enzyme . α-Arbutin produced a concentration-dependent inhibition of melanin synthesis of human melanoma cells, HMV-II . No inhibitory effect on HMV-II cell growth was seen at concentrations lower than 1.0 mM. At concentrations of 0.5 mM of arbutin, tyrosinase activity was reduced to 60% of that in non-treated cells . The addition of arbutin blocked and inhibited α-MSH-stimulated melanogenesis in B16 melanoma cells, brownish guinea pig, and human skin tissue . In a pilot study of healthy male adults exposed to UV B irradiation, topical administration of arbutin inhibited UV-induced nuclear factor-kappaB activation in human keratinocytes . In mouse skin, arbutin counteracted oxidative stress induced by 12-O-tetradecanoylphorbol-13-acetate .

PHARMACOLOGICAL ACTIONS: Tranexamic acid has a strong inhibitory effect on the activation of plasminogen, i.e. the conversion of plasminogen to plasmin, in the fibrinolytic system.The half life is 1-2 hours. Plasma protein binding is 3% at therapeutic plasma levels. The plasma protein binding seems fully accounted by its binding to plasminogen. Tranexamic acid is excreted unchanged in the urine.

PHARMACOKINETICS: Tranexamic acid is rapidly absorbed from the gastrointestinal tract. Maximum serum levels are reached within 2-3 hours. After oral administration, about 40% of the dose is excreted in the urine during the first 24 hours. After intravenous administration 45% of the dose is excreted in the urine during the first day.

Tranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. At much higher concentrations it behaves as a noncompetitive inhibitor of plasmin similar to aminocaproic acid, a similar antifibrinolytic which is 10-fold less potent. Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. In patients with hereditary angioedema, inhibition of the formation and activity of plasmin by tranexamic acid may prevent attacks of angioedema by decreasing plasmin-induced activation of the first complement protein (C1).

Off-target antagonism of GABA(A) receptors may be associated with the development of convulsions and hyperexcitability following tranexamic acid administration - the risk appears higher with improper administration or administration during cardiovascular surgery. Consider EEG monitoring of patients with a history of seizure.

Spekzo Tx Tube
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Spekzo Tx Tube
Generic	Magnesium Ascorbyl Phosphate + Kojic Acid Dipalmitate + Arbutin + Mulberry Extract + Vitamin E / Tocopherol + Tranexamic Acid
Weight	1%w/w
Type	Cream
Therapeutic Class
Manufacturer	Citaderm Pharma Pvt Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Indicated for over-the-counter use for epidermal hyperpigmentation in various skin conditions, such as melasma, freckles, and senile lentigines.

Haemorrhage or risk of haemorrhage in increased fibrinolysis or fibrinogenolysis that may occur in conditions:

Prostatectomy and bladder surgery
Menorrhagia
Epistaxis
Conisation of the cervix
Management of dental extraction in patients with coagulopathies
Ulcerative colitis
Haematuria
Gastrointestinal haemorrhage

General fibrinolysis as in prostatic and pancreatic cancer, after thoracic and other major surgery, in obstetrical complications such as abruptio placentae and post- partum haemorrhage, in leukaemia and liver diseases and in connection with thrombolytic therapy with streptokinase.

Hereditary angioneurotic oedema.

Spekzo Tx Tube is also used to associated treatment for these conditions: Mild Lower Urinary Tract InfectionBleeding, Heavy Menstrual Bleeding, Hereditary Angioedema

How Spekzo Tx Tube works

Arbutin is a hydroquinone glycoside, however the hydroquinone moiety is not solely responsible for the de-pigmentating actions of arbutin . It acts as a competitive inhibitor of tyrosinase enzyme by acting on the L-tyrosine binding site to suppress melanogenesis and mediate its de-pigmenting actions on human skin . Tyrosinase is an enzyme involved in the regulation of rate-limiting steps during the synthesis of melanin; it regulates the conversion of L-tyrosine into L-dopa, and subsequent conversion of L-dopa to L-dopaquinone . Via inhibition of tyrosinase activity in a concentration-dependent manner, arbutin attenuates the production of melanin in melanocytes. While most studies suggest that arbutin has negligible effect on the tyrosinase mRNA expression, a study assessing the effect of arbutin on melanocyte differentiation inducement system using ES cells propose that arbutin may also downregulate the expression of tyrosinase in addition to its inhibitory action on the enzyme . The contradictory findings across studies may be due to previous studies using terminally-differentiated melanocytes and melanoma cells .

Tranexamic acid competitively and reversibly inhibits the activation of plasminogen via binding at several distinct sites, including four or five low-affinity sites and one high-affinity site, the latter of which is involved in its binding to fibrin. The binding of plasminogen to fibrin induces fibrinolysis - by occupying the necessary binding sites tranexamic acid prevents this dissolution of fibrin, thereby stabilizing the clot and preventing hemorrhage.

Dosage

Spekzo Tx Tube dosage

Intravenous administration is necessary only if it is difficult to give adequate doses by mouth. The recommended standard dose is 1 to 1.5 gm or 5-10 ml by slow intravenous injection at a rate of 1 ml/minute, two to three times daily. For the indications listed below the following doses are recommended.

PROSTATECTOMY: 5-10 ml by slow intravenous injection every eight hours (the first injection being given during the operation) for the first three days after surgery; thereafter 1-1.5 gm orally three to four times daily until macroscopic haematuria is no longer present.

MENORRHAGIA: 1-1.5 gm orally three to four times daily for three to four days.

EPISTAXIS: 1.5 gm orally three times daily for four to ten days.

Tranexamic Acid injection may be applied topically to the nasal mucosa of patients suffering from epistaxis. This can be done by soaking a gauze strip in the solution,and then packing the nasal cavity.

HAEMATURIA: 1-1.5 gm orally 2-3 times daily until macroscopic haematuria is no longer present.

CONISATION OF THE CERVIX: 1.5 gm orally 3 times a day for 12 to 14 days post-operatively.

DENTAL SURGERY IN PATIENTS WITH COAGULOPATHIES: Immediately before surgery, 10 mg per kg body-weight should be given intravenously. After surgery, 25 mg per kg body-weight are given orally three to four times daily for six to eight days. Coagulation factor concentrate might be necessary to administrate.

GENERAL FIBRINOLYSIS: 1 gm by slow intravenous injection three to four times daily. With fibrinolysis in conjunction with diagnosed, increased intravascular coagulation i.e. defibrillation syndrome, an anticoagulant such as heparin may be given with caution.

HEREDITARY ANGIONEUROTIC OEDEMA: 1-1.5 gm orally two to three times daily as intermittent or continuous treatment depending on whether the patient has prodromal symptoms or not.

CHILDREN:

Oral dose: 25 mg/kg 2 to 3 times daily for 7 to 10 days.
Injection: 10 mg/kg 6 to 8 hours for 7 to 10 days

Side Effects

Dose-dependent, gastrointestinal discomfort is the most commonly reported undesirable effect, but it is usually of mild and temporary in nature. Allergic skin reactions have been reported as an uncommon undesirable effect. Hypotension may occur after fast injection.

Toxicity

In an acute oral toxicity study, the LD50-value for β-arbutin is 9804 mg/kg bw for the mouse and 8715 mg/kg bw for the rat . Dermal LD50 value in rat and mouse was reported to be greater than 928 mg/kg bw, according to an acute dermal toxicity study . Extremely high doses may cause ringing in the ears, shortness of breath, convulsions, collapse, vomiting and delirium . Nausea and vomiting were seen individuals with sensitive stomachs following oral ingestion of 15 g of dried uva ursi leaves that contain arbutin .

Reported symptoms of tranexamic acid overdose include severe gastrointestinal symptoms, hypotension, thromboembolism, visual impairment, convulsions, mental status changes, and rash.

Precaution

Patients with irregular menstrual bleeding, patients with a high risk of thrombosis (a previous thromboembolic event and a family history of thromboembolic disease) should use it only if there is a strong medical indication and under strict medical supervision.

Patients with disseminated intravascular coagulation (DIC), who require treatment with it must be under the strict supervision of a physician experienced in treating this disorder.

In the long-term treatment of patients, regular eye examination should be performed. If a colour vision disorder should occur during the course of treatment, the drug should be discontinued.

Interaction

Clinically important interactions have not been observed with Tranexamic acid. Because of the absence of interaction studies, simultaneous treatment with anticoagulants must take place under the strict supervision of a physician experienced in this field.

Volume of Distribution

No pharmacokinetic data available.

The initial volume of distribution of tranexamic acid is 0.18 L/kg and its steady-state volume of distribution is 0.39 L/kg. Tranexamic acid distributes into cerebrospinal fluid and the aqueous humor of the eye at concentrations approximately 1/10th of typical plasma concentrations. Tranexamic acid is also able to cross the placenta, found in cord blood at concentrations equivalent to maternal plasma concentrations.

Elimination Route

Arbutin was found to be extensively absorbed from the gastrointestinal tract where it is primarily converted to hydroquinone .

The bioavailability of tranexamic acid after oral administration in humans is approximately 30 to 50% of the ingested dose and is not affected by food intake. The C_max and T_max following multiple oral doses (1300 mg three times daily x 5 days) were 16.41 mcg/mL and 2.5 h, respectively.

Half Life

No pharmacokinetic data available.

Following intravenous administration, the apparent elimination half-life is approximately 2 hours and the mean terminal half-life is approximately 11 hours.

Clearance

No pharmacokinetic data available.

The plasma clearance of tranexamic acid is 110-116 mL/min.

Elimination Route

During the first 4 hours following ingestion of a single dose of 210 mg arbutin in healthy volunteers, 224.5 μmol/L hydroquinone glucuronide and 182 μmol/L of hydroquinone sulfate were recovered in the urine .

Urinary excretion is the primary means of tranexamic acid elimination, with >95% of an administered dose excreted in the urine as unchanged parent drug. The rate of excretion is dependent on the route of administration - approximately 90% of an intravenously administered dose is excreted within 24 hours whereas only 39% of an orally administered dose is excreted within the same time frame.

Pregnancy & Breastfeeding use

Pregnancy: Tranexamic acid crosses the placenta. Clinical experience of use in pregnant women is limited. Animal studies have not supplied any evidence of an increased incidence of fetal damage.

Lactation: Tranexamic acid is excreted into breast milk, but it is not likely to influence the child at therapeutic doses.

Contraindication

Active thromboembolic disease, such as deep vein thrombosis, pulmonary embolism and cerebral thrombosis
Subarachnoid haemorrhage
Hypersensitivity to Tranexamic acid or any of the ingredients

Special Warning

Renal Impairment:

Intravenous : Adjust dose based on the serum-creatinine concentration:

120-250 micromol/l: 10 mg/kg bid daily;
250-500 micromoles/l: 10 mg/kg once daily;
>500 micromol/l: 5 mg/kg once daily or 10 mg/kg once every 48 hr.

Oral : Adjust dose based on serum creatinine concentration:

120-250 micromol/l: 15 mg/kg bid daily;
250-500 micromol/l: 15 mg/kg once daily;
>500 micromol/l: 7.5 mg/kg once daily or 15 mg/kg once every 48 hr.

Pediatric Use: The drug has had limited use in pediatric patients, principally in connection with tooth extraction. The limited data suggest that dosing instructions for adults can be used for pediatric patients needing Tranexamic acid therapy.

Geriatric Use: Clinical studies of Tranexamic acid did not include sufficient numbers of subjects aged 65 and over to determine whether they respond different y from younger subjects. Other reported clinical experien e has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function. Drug Interaction Tranexamic Acid is known to interact with other drugs like Factor VIII. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required. Pharmaceutical Precaution Keep in a cool & dry place, protected from light. Keep out of the reach of children.