Description

Composition:
Each Speedex-TH+ tablet contains:
Paracetamol 325mg
Aceclofenac 100mg
Thiocolchicoside 4mg
 
Dosage form:
Tablets
 
ATC classification:
Analgesic and muscle relaxant
 
Description: 
Speedex-TH+ tablets have the time tested combination formulated to provide speedy relief from pain, muscular spasms and inflammation associated with muscoskeletal and neuromuscular conditions. Paracetamol, the analgesic and antipyretic component of Speedex-TH+ shows synergistic effect with aceclofenac present in the formulation. Aceclofenac has more specific action and greater tolerability, lesser gastric ulcerogenicity compared to that of other non-steroidal anti- inflammatory drugs. Thiocolchicoside is the centrally acting muscle relaxant that has better tolerability even for long term treatments. It also has anti-inflammatory and analgesic activity. It modulates the chemical mediators of inflammation by which it interferes with the initiation and amplification of the joint inflammation. Combination of thiocolchicoside with two other analgesics makes the comprehensive formula of Speedex-TH+ satisfactory in prescribing for arthritis.
 
Pharmacological action:
Paracetamol shows analgesic effect by elevating pain threshold which is thought to be attained by inhibiting nitric oxide pathway mediated by a variety of neurotransmitter receptors including N-methyl-D aspartate (NMDA) and substance P. It shows antipyretic activity by inhibiting the synthesis and release of prostaglandin in the central nervous system, thereby inhibiting prostaglandin-mediated effects on the heat-regulating center in the anterior hypothalamus.
Aceclofenac, after absorption undergoes intracellular metabolism to 4’ hydroxy-aceclofenac and diclofenac in human rheumatoid synovial cells and other inflammatory cells. These metabolites inhibit the enzyme, cyclooxygenase (COX-1 & COX-2), an early component of the arachidonic acid cascade that results in the formation of mediators of pain and inflammation: prostaglandins, thromboxanes and prostacyclins. In human osteoarthritic synovial cells and human articular chondrocytes, these metabolites inhibit the formation of inflammatory mediators such as IL-1β, IL-6 and tumor necrosis factor which are implicated in arthritis. Aceclofenac promotes bone cartilage matrix synthesis by stimulating glycosaminoglycan synthesis and suppresses cartilage degeneration by inhibiting IL-1β.
Thiocolchicoside acts on the muscular contracture by antagonizing the receptors of neurotransmitters ɣ-amino-butyric acid (GABA) and glycine present in CNS. It is a competitive antagonist of GABAA receptor, exerting its muscle relaxant effect at supra-spinal level via complex regulatory mechanisms.
 
Pharmacokinetics:
Paracetamol:
It is absorbed rapidly mainly from the small intestine producing peak plasma levels after 15-20 minutes following oral dosing.  Its systemic bioavailability is dose-dependent and ranges from 70 to 90%. Food delays oral absorption. It is rapidly and widely distributed throughout the body with a volume of distribution of approximately 0.9L/kg and is eliminated from plasma with a half life of approximately 2 hours. It is extensively metabolised predominantly in the liver, the major metabolites being the sulphate and glucuronide conjugates which are excreted in urine.
Aceclofenac:
Following oral administration of Aceclofenac peak plasma concentrations (Cmax) are reached after 1-3 hours and it has plasma elimination half life of approximately 4 hours. Volume of distribution (Vd) is approximately 25 liters and it is more than 99% bound to plasma proteins. In patients with knee pain, swelling and synovial fluid effusion, the plasma concentration of Aceclofenac was found to be twice that in synovial fluid after multiple doses of the drug. Renal excretion is the primary mode of elimination where 70-80% of administered dose of Aceclofenac was found in urine as glucoronides
Thiocolchicoside:
After oral administration, no thiocolchicoside is detected in plasma indicating an intestinal metabolism. Of the two circulating metabolites one is pharmacologically active and both the metabolites reach the maximum plasma concentrations 1hour after administration of thiocolchicoside. The drug is primarily eliminated via feces and the rest undergoes renal elimination.
 
Indications:
Speedex-TH+ is indicated for the following
¬ Painful muscle contractures in acute spinal pathology in adults and adolescents from 16 years onwards
¬ Acute disc prolapse
¬ Acute low back pain
¬ Severe muscoskeletal pain due to trauma or injury
¬ Sprain and strains
¬ Cervical pain
¬ Muscle spasms
¬ Pain and inflammation due to ankylosing spondylitis and spondyloarthritis
¬ Pain due to osteoarthritis, rheumatoid arthritis and gout attacks
¬ Pain and inflammation due to sports injuries
¬ Pain associated with cervical root and disc syndromes.
¬ Myalgias, torticollis and fibrositis.
 
Dosage and Administration:
Recommended dosage unless otherwise specified by Physician:
For adults and children above 16yrs:
1 Speedex-TH+ tablet two-three times in a day. The treatment duration is limited to 7 consecutive days.
 
Contraindications:
¬ Speedex-TH+ is contraindicated in patients with hypersensitivity or idiosyncrasy to any of its ingredients and NSAIDs
¬ Thiocolchicoside present in Speedex-TH+ has powerful convulsant activity and should not be used in seizure prone individuals.
¬ In patients with GI bleeding, moderate to severe renal impairment and acute porphyria
¬ Speedex-TH+ must not be used during the entire pregnancy period, during lactation and in women of childbearing potential not using contraception.
¬ Patients in whom aspirin or other NSAIDs, precipitate attacks of bronchospasm, urticaria or acute rhinitis.
¬ Patients with severe heart failure, hypertension, hepatic or renal insufficiency.
 
Side effects:
The common adverse effects are:
Sedation, drowsiness, blurred or double vision, nausea, heartburn, diarrhea, headache, dizziness, fluid and salt retention, edema feet, high blood pressure, flatulence, constipation, abdominal pain and loss of appetite.
Discontinue use if any hypersensitivity reactions such as rash or redness occur.
 
Warnings and Precautions:
Special Warning and Precaution:
Preclinical studies of thiocolchicoside showed that one of thiocolcoside metabolites (SL59.0955) induced aneuploidy (i.e. unequal number of chromosomes in dividing cells) at concentrations close to human exposure observed at doses 8 mg twice daily). Aneuploidy is considered as a risk factor for teratogenicity, embryo toxicity fetal toxicity, spontaneous abortion, and impaired male fertility and a potential risk factor for cancer. As a precautionary measure, use of the product at doses exceeding the recommended dose or long-term use should be avoided. Patients of childbearing potential not using contraception, who are on this medication, should be carefully informed about the potential risk in the pregnancy and about effective contraception measures to be followed.
General Warnings and Precautions:
¬ Inform your doctor if you are on any pain killers/NSAIDs.
¬ Drowsiness can occur with the use of Speedex-TH+ and may be additive to drowsiness from the concomitant use of alcohol or other central nervous system depressants.
¬ It is recommended to avoid use of machinery or driving when on this medication.
¬ Speedex-TH+ might increase the risk of serious cardiovascular events or intestinal bleeding. Ensure that you fully discuss the potential risks with your physician before beginning treatment.
¬ If you suffer from liver disease and gastrointestinal disorders, ensure that you make your physician aware of this before treatment begins, in order for your physician to determine whether or not this medicine is safe and suitable for you.
¬ Precaution to be exercised in patients with: Gastrointestinal bleeding, history of peptic ulceration, cerebrovascular bleeding, ulcerative colitis, Crohn’s disease, systematic lupus erythromatosus (SLE), porphyria, hematopoietic or coagulation disorders, Raynaud’s phenomenon.
Drug Interactions:
¬ The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by cholestyramine. The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular daily use of paracetamol with increased risk of bleeding; however occasional doses have no significant effect.
¬ Diclofenac may increase the plasma concentrations of lithium & digoxin. Concomitant use of diclofenac & diuretics may inhibit the activity of diuretics. The activity of anticoagulants may be enhanced when used concomitantly with diclofenac. It may increase toxicity of drugs like cyclosporine. NSAIDs may diminish anti-hypertensive action of ACE-inhibitors.
¬ Thiocolchicoside is a centrally acting muscle relaxant with convulsant activity in seizure prone individuals hence patients on medications that have CNS effects should be given Speedex-TH+ only after thorough evaluation.
Pregnancy and Lactation:
Category C
Speedex-TH+ is contraindicated during pregnancy and in women of childbearing potential not using contraception
Since thiocolchicoside passes into the mother’s milk, its use is contraindicated during breastfeeding.
Pediatric use:
Safety and efficacy of Speedex-TH+ in pediatric patients has not been established.
 
References:
Paracetamol-https://pubchem.ncbi.nlm.nih.gov/compound/acetaminophen#section=Top
Thiocolchicoside
https://pubchem.ncbi.nlm.nih.gov/compound/Coltramyl
https://books.google.co.in/books?id=FfG8AQAAQBAJ&pg=PA358&dq=thiocolchicoside+pharmacology&hl=en&sa=X&redir_esc=y#v=onepage&q=thiocolchicoside%20pharmacology&f=false
Thiocolchicoside as muscle relaxant: a review
https://pdfs.semanticscholar.org/6848/43f3f7ad8f393bd283e514563a8a0e8141f1.pdf
Aceclofenac:
https://pubchem.ncbi.nlm.nih.gov/compound/Aceclofenac
 
Disclaimer:

• Information provided above is for reference purpose only and has been compiled for use by healthcare practitioners. Please consult your physician to understand how the product affects you, its dosages, side-effects and further information.
• Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indications prescribed by your physician.
• Every effort has been made to ensure that the information provided by Pharma Synth Formulations Ltd. (‘PSFL’) is accurate, up-to-date, and complete, but no guarantee is made to that effect. PSFL does not endorse drugs, diagnose patients or recommend therapy and is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. PSFL does not assume any responsibility for any aspect of healthcare administered with the aid of information provided. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.