ATC Group: V03A All other therapeutic products

Acetylcysteine is N-acetyl derivative of cysteine. Used as a mucolytic agent to reduce the viscosity of mucous secretions.

Amifostine is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite. This metabolite is believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues.

Andexanet alfa is a recombinant form of human FXa protein that has been modified to lack FXa enzymatic activity. Andexanet alfa is a specific reversal agent for FXa inhibitors. The predominant mechanism of action is the binding and sequestration of the FXa inhibitor. In addition, andexanet alfa has been observed to bind to, and inhibit tissue factor pathway inhibitor (TFPI). Inhibition of TFPI activity can increase tissue factor-initiated thrombin generation inducing a pro-coagulant effect.

Benserazide (also called Serazide or Ro 4-4602) is a peripherally acting aromatic L-amino acid decarboxylase or DOPA decarboxylase inhibitor, which is unable to cross the blood–brain barrier.

Calcium is an endogenous ion of the body essential for the maintenance of a number of physiologic processes. It participates as an integral factor in the maintenance of the functional integrity of the nervous system, in the contractile mechanisms of muscle tissue, in the clotting of blood, and in the formation of the major structural material of the skeleton. Soluble calcium salts are commonly used in the treatment of calcium deficiency.

Calcium folinate is an active metabolite of folinic acid and essential coenzyme for nucleic acid synthesis in cytotoxic therapy. Calcium folinate is frequently used to diminish the toxicity and counteract the action of folate antagonists, such as methotrexate.

Carbidopa is a peripheral aromatic amino acid decarboxylase inhibitor. It prevents metabolism of levodopa to dopamine in the peripheral circulation, ensuring that a higher proportion of the dose reaches the brain, where dopamine exerts its therapeutic effects. A lower dose of levodopa can be used when it is coadministered with carbidopa, reducing the incidence and severity of peripheral side effects.

Cobicistat is a mechanism-based inhibitor of cytochromes P450 of the CYP3A subfamily. Inhibition of CYP3A-mediated metabolism by cobicistat enhances the systemic exposure of CYP3A substrates, such as darunavir, where bioavailability is limited and half-life is shortened due to CYP3A-dependent metabolism.

Colestilan is a non-absorbed, non-calcium, non-metallic phosphate-binding polymer. The binding sites become partially protonated in the stomach and interact through ionic and hydrogen bonding with both dietary phosphate anions and bile acids in the duodenum. By binding phosphate from food in the digestive tract, colestilan lowers the serum phosphorus concentration. Colestilan also binds bile acids, thereby lowering the serum LDL-cholesterol concentration.

Deferasirox is an orally active chelator that is highly selective for iron (III). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Deferasirox promotes excretion of iron, primarily in the faeces.

Deferiprone is a bidentate ligand which binds iron in a 3:1 molar ratio. Deferiprone monotherapy is indicated for the treatment of iron overload in patients with thalassaemia major when current chelation therapy is contraindicated or inadequate.

Deferoxamine is a chelating agent for trivalent iron and aluminium ions. The resulting chelates are stable and non-toxic.

Dexrazoxane has two major mechanisms of action, chelation of iron and inhibition of topoisomerase II. It is not known to what extent each of these mechanisms contributes to the preventive effect on tissue destruction following anthracycline extravasation.

Diazoxide is a peripheral vasodilator and has qualitatively the same effect on blood vessels as benzothiazine compounds, but the effect is more rapid and profound. Unlike benzothiazines, diazoxide is non-diuretic and causes retention of sodium and water. It causes a prompt increase in blood glucose by a direct inhibitory action on the secretion of insulin by the beta cells in the Islets of Langerhans.

Cyanide blocks intracellular respiration by binding to cytochrome oxidase. Dicobalt edetate forms a stable complex with the cyanide thereby acting as an antidote.

Difelikefalin is a selective kappa opioid receptor agonist with low central nervous system penetration. The pathophysiology of chronic kidney disease-associated pruritus is thought to be multifactorial, including systemic inflammation and an imbalance in the endogenous opioid system (e.g., overexpression of mu opioid receptors and concomitant downregulation of kappa opioid receptors). The activation of kappa opioid receptors on peripheral sensory neurons and immune cells by difelikefalin are considered mechanistically responsible for the antipruritic and anti-inflammatory effects.

Dimercaprol is a chelating agent used in the treatment of acute poisoning by heavy metals.

Ethanol is an organic compound used in medical wipes and most commonly in antibacterial hand sanitizer gels as an antiseptic for its bactericidal and anti-fungal effects. Ethanol kills microorganisms by dissolving their membrane lipid bilayer and denaturing their proteins, and is effective against most bacteria, fungi and viruses. Ethanol also blocks conduction in peripheral nerve by decreasing the maximal values of both the sodium and potassium conductances and has a depressant action on the vasomotor-centre.

When the vapour is inhaled eucalyptus oil acts to ventilate the bronchial passages and relieve bronchitis and associated conditions. It is also a rubefacient.

Ferric citrate is a phosphate binder and iron replacement product. It is used for the control of serum phosphorus levels and the treatment of iron deficiency anemia in adult patients with chronic kidney disease on dialysis.

Flumazenil, an imidazobenzodiazepine, is a benzodiazepine antagonist which, by competitive interaction, blocks the effects of substances acting via the benzodiazepine-receptor. Neutralisation of paradoxal reactions of benzodiazepines has been reported.

Fomepizole is a competitive inhibitor of alcohol dehydrogenase. Alcohol dehydrogenase catalyzes the oxidation of ethanol to acetaldehyde and the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Fomepizole is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning (such as windshield washer fluid), or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis.

The standardised ginseng extract G115 raises the general level of cellular activity, which is expressed by a pronounced increase in the physical and mental capacity.

Glucarpidase is a recombinant bacterial enzyme that hydrolyses the carboxyl-terminal glutamate residue from folic acid and structurally related molecules such asMTX. Glucarpidase converts MTX to its inactive metabolites DAMPA and glutamate.

Idarucizumab is a humanized monoclonal antibody fragment (Fab) that binds to dabigatran with very high affinity, approximately 300-fold more potent than the binding affinity of dabigatran for thrombin. The idarucizumab-dabigatran complex is characterised by a rapid on-rate and extremely slow off-rate resulting in a very stable complex. Idarucizumab potently and specifically binds to dabigatran and its metabolites and neutralises their anticoagulant effect.

Ipecacuanha root extract has been widely used in syrup form as a potent and effective emetic. Ipecacuanha powder had been used to induce sweating at the onset of influenza, and small amounts of the extract have been incorporated into cough syrups as expectorants.

Iron sucrose is composed of a polynuclear iron(III)-hydroxide core surrounded by a large number of non-covalently bound sucrose molecules. The polynuclear iron core has a structure similar to that of the core of the physiological iron storage protein ferritin. The complex is designed to provide, in a controlled manner, utilisable iron for the iron transport and storage proteins in the body (i.e., transferrin and ferritin, respectively).

Lanthanum is indicated as a phosphate binding agent for use in the control of hyperphosphataemia.

Levoleucovorin is the pharmacologically active isomer of 5-formyltetrahydrofolic acid. Administration of levoleucovorin can “rescue” normal cells and thereby prevent toxicity of folic acid antagonists such as methotrexate which act by inhibiting dihydrofolate reductase.

Mesna is an antidote, and offers the possibility of reliably preventing urotoxic side-effects associated with aggressive cancer chemotherapy using oxazaphosphorine cytostatics.

In vivo, in low concentration, methylthioninium chloride speeds up the conversion of methaemoglobin to haemoglobin. Methylthioninium chloride has been observed to stain tissues selectively.

Naloxone hydrochloride, a semisynthetic morphine derivative (N-allyl-nor-oxymorphone), is a specific opioid antagonist that acts competitively at opioid receptors. It reveals very high affinity for the opioid receptor sites and therefore displaces both opioid agonists and partial antagonists, such as pentazocine, for example, but also nalorphine.

Oxygen is an essential element for living organisms. It is involved in cellular metabolism and catabolism and permits production of energy in the form of adenosine triphosphate (ATP). The variation of the partial pressure of oxygen in the blood affects the cardiovascular system, the respiratory system, cellular metabolism, and the central nervous system. Deprivation of oxygen, resulting in tissue hypoxia, results in a rapid deterioration of myocardial and central nervous activity. Intervention with oxygen therapy is essential for the resolution of adequate tissue oxygenation.

Papain is a proteolytic enzyme extracted from the raw fruit of the papaya plant (Carica papaya). Papain catalyzes the breakdown of proteins by hydrolysis (addition of a water molecule).

Patiromer is a non-absorbed, cation exchange polymer that contains a calcium-sorbitol complex as a counterion. Patiromer increases faecal potassium excretion through binding of potassium in the lumen of the gastrointestinal tract. Binding of potassium reduces the concentration of free potassium in the gastrointestinal lumen, resulting in a reduction of serum potassium levels.

Phentolamine is a competitive non-selective α₁- and α₂-adrenergic receptor blocker of relatively short duration of action. It causes vasodilatation and a fall in blood pressure resulting from the blockade of both post-junctional vascular α₁- and α₂-adrenoceptors. It also antagonises the vasoconstrictor response to noradrenaline and adrenaline infusions.

Physostigmine is a reversible inhibitor of acetylcholinesterase. As an inhibitor of acetyl-cholinesterase, physostigmine slows down the degradation of acetylcholine and acts like an indirect parasympathomimetic drug due to an increase of the acetylcholine concentration at the receptor.

Potassium iodide is indicated as a thyroid-blocking agent to prevent the uptake of radioactive iodine, for example after a nuclear accident or during a nuclear medicine investigation before administering a radioiodinated compound, which is metabolised to iodide or which contains radioiodine impurities.

Protamine is a potent antidote for heparin. Its precise mechanism of action is unknown. However, when the strongly basic protamine combines with the strongly acid heparin, a stable salt is formed lacking in anticoagulant activity.

Prussian blue insoluble binds cesium and thallium isotopes in the gastrointestinal tract after these isotopes are ingested or excreted in the bile by the liver, thereby reducing gastrointestinal reabsorption (enterohepatic circulation).

Rasburicase is a highly potent uricolytic agent that catalyses enzymatic oxidation of uric acid into allantoin, a water soluble product, easily excreted by the kidneys in the urine.

Sevelamer is a non-absorbed phosphate binding crosslinked polymer, free of metal and calcium. Sevelamer contains multiple amines separated by one carbon from the polymer backbone which become protonated in the stomach. These protonated amines bind negatively charged ions such as dietary phosphate in the intestine.

Sodium folinate is a reduced derivative of folic acid. Sodium folinate is mainly used for colorectal cancer treatment in association with 5-fluorouracil and Oxaliplatin (FOLFOX regimen) or with 5-fluorouracil and Irinotecan (FOLFIRI regimen). Additionally, it is administered as salvage therapy to reduce toxic effects following high doses of methotrexate in the treatment of some neoplastic diseases, rheumatoid arthritis or severe psoriasis. Sodium folinate is also given to treat anemia caused by folate deficiency.

Sodium levofolinate is the pharmacologically active isomer of 5-formyl tetrahydrofolic acid. Sodium levofolinate does not require reduction by dihydrofolate reductase to participate in reactions utilizing folates as a source of “one-carbon” moieties. Administration of levoleucovorin counteracts the therapeutic and toxic effects of folic acid antagonists such as methotrexate, which act by inhibiting dihydrofolate reductase.

Sodium nitrite is indicated for sequential use with sodium thiosulfate for the treatment of acute cyanide poisoning that is judged to be life-threatening. Sodium nitrite is thought to exert its therapeutic effect by reacting with hemoglobin to form methemoglobin, an oxidized form of hemoglobin incapable of oxygen transport but with high affinity for cyanide.

Sodium zirconium cyclosilicate is a non-absorbed, non-polymer inorganic powder with a uniform micropore structure that preferentially captures potassium in exchange for hydrogen and sodium cations. Sodium zirconium cyclosilicate captures potassium throughout the entire gastrointestinal (GI) tract and reduces the concentration of free potassium in the GI lumen, thereby lowering serum potassium levels and increasing faecal potassium excretion to resolve hyperkalaemia.

Succimer is a lead chelator; it forms water soluble chelates and, consequently, increases the urinary excretion of lead.

Sucroferric oxyhydroxide is also known as a mixture of polynuclear iron(III)-oxyhydroxide (pn-FeOOH), sucrose and starches. Phosphate binding takes place by ligand exchange between hydroxyl groups and/or water and the phosphate ions throughout the physiological pH range of the gastrointestinal tract. Serum phosphorus levels are reduced as a consequence of the reduced dietary phosphate absorption.

Sugammadex is a modified gamma cyclodextrin which is a Selective Relaxant Binding Agent. It forms a complex with the neuromuscular blocking agents rocuronium or vecuronium in plasma and thereby reduces the amount of neuromuscular blocking agent available to bind to nicotinic receptors in the neuromuscular junction.

Sodium thiosulfate is indicated for sequential use with sodium nitrite for the treatment of acute cyanide poisoning that is judged to be life-threatening. The primary route of endogenous cyanide detoxification is by enzymatic transulfuration to thiocyanate (SCN-), which is relatively nontoxic and readily excreted in the urine.

Sodium thiosulfate is also indicated for the prevention of ototoxicity induced by cisplatin chemotherapy. The mechanism of protection against ototoxicity may include increasing levels of endogenous antioxidants, inhibition of intracellular oxidative stress, and direct interaction between cisplatin and the thiol group in sodium thiosulfate to produce inactive platinum species.

Hydroxocobalamin is a cyanide antidote. Its action in the treatment of cyanide poisoning is based on its ability to bind cyanide ions. Each hydroxocobalamin molecule can bind one cyanide ion by substituting it for the hydroxo ligand linked to the trivalent cobalt ion, to form cyanocobalamin, which is then excreted in the urine.