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Eflornithine
Eflornithine, sold under the brand name Vaniqa among others, is a medication used to treat African trypanosomiasis (sleeping sickness) and excessive hair growth on the face in women. Specifically it is used for the 2nd stage of sleeping sickness caused by '' T. b. gambiense'' and may be used with nifurtimox. It is taken intravenously (injection into a vein) or topically. It has also been given orally on at least some rare occasions for the treatment of African trypanosomiasis. Common side effects when applied as a cream include rash, redness, and burning. Side effects of the injectable form include bone marrow suppression, vomiting, and seizures. It is unclear if it is safe to use during pregnancy or breastfeeding. It is recommended typically for children over the age of 12. Eflornithine was developed in the 1970s and came into medical use in 1990. It is on the World Health Organization's List of Essential Medicines. In the United States the injectable form can be obtained ...
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Nifurtimox-eflornithine Combination Treatment
Nifurtimox/eflornithine is a combination of two antiparasitic drugs, nifurtimox and eflornithine, used in the treatment of African trypanosomiasis (sleeping sickness). It is included in the World Health Organization The World Health Organization (WHO) is a specialized agency of the United Nations responsible for international public health. The WHO Constitution states its main objective as "the attainment by all peoples of the highest possible level o ...'s Model List of Essential Medicines. A treatment regimen known as nifurtimox-eflornithine combination treatment (NECT) is used in second stage gambiense African trypanosomiasis throughout Africa where the disease is endemic. The regimen involves slow infusion of 400 mg of eflornithine every 12 hours for 7 days combined with 15 mg/kg of nifurtimox orally three times a day for 10 days. References {{reflist Antiparasitic agents ...
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African Trypanosomiasis
African trypanosomiasis, also known as African sleeping sickness or simply sleeping sickness, is an insect-borne parasitic infection of humans and other animals. It is caused by the species '' Trypanosoma brucei''. Humans are infected by two types, ''Trypanosoma brucei gambiense'' (TbG) and ''Trypanosoma brucei rhodesiense'' (TbR). TbG causes over 98% of reported cases. Both are usually transmitted by the bite of an infected tsetse fly and are most common in rural areas. Initially, the first stage of the disease is characterized by fevers, headaches, itchiness, and joint pains, beginning one to three weeks after the bite. Weeks to months later, the second stage begins with confusion, poor coordination, numbness, and trouble sleeping. Diagnosis is by finding the parasite in a blood smear or in the fluid of a lymph node. A lumbar puncture is often needed to tell the difference between first- and second-stage disease. If the disease is not treated quickly it can lead to death. ...
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Nifurtimox
Nifurtimox, sold under the brand name Lampit, is a medication used to treat Chagas disease and sleeping sickness. For sleeping sickness it is used together with eflornithine in nifurtimox-eflornithine combination treatment. In Chagas disease it is a second-line option to benznidazole. It is given by mouth. Common side effects include abdominal pain, headache, nausea, and weight loss. There are concerns from animal studies that it may increase the risk of cancer but these concerns have not been found in human trials. Nifurtimox is not recommended in pregnancy or in those with significant kidney or liver problems. It is a type of nitrofuran. Nifurtimox came into medication use in 1965. It is on the World Health Organization's List of Essential Medicines. It is not available commercially in Canada. It was approved for medical use in the United States in August 2020. In regions of the world where the disease is common nifurtimox is provided for free by the World Health Organizati ...
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Ornithine Decarboxylase
The enzyme ornithine decarboxylase (, ODC) catalyzes the decarboxylation of ornithine (a product of the urea cycle) to form putrescine. This reaction is the committed step in polyamine synthesis. In humans, this protein has 461 amino acids and forms a homodimer. Reaction mechanism Lysine 69 on ornithine decarboxylase (ODC) binds the cofactor pyridoxal phosphate to form a Schiff base. Ornithine displaces the lysine to form a Schiff base attached to orthonine, which decarboxylates to form a quinoid intermediate. This intermediate rearranges to form a Schiff base attached to putrescine, which is attacked by lysine to release putrescine product and reform PLP-bound ODC. This is the first step and the rate-limiting step in humans for the production of polyamines, compounds required for cell division. Structure image:Ornithine Decarboxylase Publication View.png, 270px, 3D crystal structure of ornithine decarboxylase.; ; rendered viPyMOL The active form of ornithine ...
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Melarsoprol
Melarsoprol is an arsenic-containing medication used for the treatment of sleeping sickness (African trypanosomiasis). It is specifically used for second-stage disease caused by ''Trypanosoma brucei rhodesiense'' when the central nervous system is involved. For ''Trypanosoma brucei gambiense'', eflornithine or fexinidazole is usually preferred. It is effective in about 95% of people. It is given by injection into a vein. Melarsoprol has a high number of side effects. Common side effects include brain dysfunction, numbness, rashes, and kidney and liver problems. About 1-5% of people die during treatment, although this is tolerated due to sleeping sickness itself having a practically 100% mortality rate when untreated. In those with glucose-6-phosphate dehydrogenase (G6PD) deficiency, red blood cell breakdown may occur. It has not been studied in pregnancy. It works by blocking pyruvate kinase, an enzyme required for aerobic metabolism by the parasite. Melarsoprol has been used ...
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Trypanosoma Brucei
''Trypanosoma brucei'' is a species of parasitic kinetoplastid belonging to the genus '' Trypanosoma'' that is present in sub-Saharan Africa. Unlike other protozoan parasites that normally infect blood and tissue cells, it is exclusively extracellular and inhabits the blood plasma and body fluids. It causes deadly vector-borne diseases: African trypanosomiasis or sleeping sickness in humans, and animal trypanosomiasis or ''nagana'' in cattle and horses. It is a species complex grouped into three subspecies: ''T. b. brucei'', ''T. b. gambiense'' and ''T. b. rhodesiense''. The first is a parasite of non-human mammals and causes ''nagana'', while the latter two are zoonotic infecting both humans and animals and cause African trpanosomiasis. ''T. brucei'' is transmitted between mammal hosts by an insect vector belonging to different species of tsetse fly (''Glossina''). Transmission occurs by biting during the insect's blood meal. The parasites undergo complex morphological chan ...
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Hirsutism
Hirsutism is excessive body hair on parts of the body where hair is normally absent or minimal. The word is from early 17th century: from Latin ''hirsutus'' meaning "hairy". It usually refers to a "male" pattern of hair growth in a female that may be a sign of a more serious medical condition, especially if it develops well after puberty. Cultural stigma against hirsutism can cause much psychological distress and social difficulty. Discrimination based on facial hirsutism often leads to the avoidance of social situations and to symptoms of anxiety and depression. Hirsutism is usually the result of an underlying endocrine imbalance, which may be adrenal, ovarian, or central. It can be caused by increased levels of androgen hormones. The amount and location of the hair is measured by a Ferriman-Gallwey score. It is different from hypertrichosis, which is excessive hair growth anywhere on the body. Treatments may include certain birth control pills, antiandrogens, or insuli ...
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WHO Model List Of Essential Medicines
The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health system. The list is frequently used by countries to help develop their own local lists of essential medicines. , more than 155 countries have created national lists of essential medicines based on the World Health Organization's model list. This includes both developed and developing countries. The list is divided into core items and complementary items. The core items are deemed to be the most cost-effective options for key health problems and are usable with little additional health care resources. The complementary items either require additional infrastructure such as specially trained health care providers or diagnostic equipment or have a lower cost–benefit ratio. About 25% of items are in the complementary list. Some medicat ...
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Decarboxylation
Decarboxylation is a chemical reaction that removes a carboxyl group and releases carbon dioxide (CO2). Usually, decarboxylation refers to a reaction of carboxylic acids, removing a carbon atom from a carbon chain. The reverse process, which is the first chemical step in photosynthesis, is called carboxylation, the addition of CO2 to a compound. Enzymes that catalyze decarboxylations are called decarboxylases or, the more formal term, carboxy-lyases ( EC number 4.1.1). In organic chemistry The term "decarboxylation" usually means replacement of a carboxyl group () with a hydrogen atom: :RCO2H -> RH + CO2 Decarboxylation is one of the oldest known organic reactions. It is one of the processes assumed to accompany pyrolysis and destructive distillation. Metal salts, especially copper compounds, facilitate the reaction via the intermediacy of metal carboxylate complexes. Decarboxylation of aryl carboxylates can generate the equivalent of the corresponding aryl anion, which ...
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Transamination
Transamination is a chemical reaction that transfers an amino group to a ketoacid to form new amino acids. This pathway is responsible for the deamination of most amino acids. This is one of the major degradation pathways which convert essential amino acids to non-essential amino acids (amino acids that can be synthesized de novo by the organism). Transamination in biochemistry is accomplished by enzymes called transaminases or aminotransferases. α-ketoglutarate acts as the predominant amino-group acceptor and produces glutamate as the new amino acid. :Aminoacid + α-ketoglutarate ↔ α-keto acid + glutamate Glutamate's amino group, in turn, is transferred to oxaloacetate in a second transamination reaction yielding aspartate. :Glutamate + oxaloacetate ↔ α-ketoglutarate + aspartate Mechanism of action Transamination catalyzed by aminotransferase occurs in two stages. In the first step, the α amino group of an amino acid is transferred to the enzyme, producing t ...
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Seizures
An epileptic seizure, informally known as a seizure, is a period of symptoms due to abnormally excessive or synchronous neuronal activity in the brain. Outward effects vary from uncontrolled shaking movements involving much of the body with loss of consciousness ( tonic-clonic seizure), to shaking movements involving only part of the body with variable levels of consciousness ( focal seizure), to a subtle momentary loss of awareness ( absence seizure). Most of the time these episodes last less than two minutes and it takes some time to return to normal. Loss of bladder control may occur. Seizures may be provoked and unprovoked. Provoked seizures are due to a temporary event such as low blood sugar, alcohol withdrawal, abusing alcohol together with prescription medication, low blood sodium, fever, brain infection, or concussion. Unprovoked seizures occur without a known or fixable cause such that ongoing seizures are likely. Unprovoked seizures may be exacerbated by stress ...
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Thrombocytopenia
Thrombocytopenia is a condition characterized by abnormally low levels of platelets, also known as thrombocytes, in the blood. It is the most common coagulation disorder among intensive care patients and is seen in a fifth of medical patients and a third of surgical patients. A normal human platelet count ranges from 150,000 to 450,000 platelets/microliter (μl) of blood. Values outside this range do not necessarily indicate disease. One common definition of thrombocytopenia requiring emergency treatment is a platelet count below 50,000/μl. Thrombocytopenia can be contrasted with the conditions associated with an abnormally ''high'' level of platelets in the blood - thrombocythemia (when the cause is unknown), and thrombocytosis (when the cause is known). Signs and symptoms Thrombocytopenia usually has no symptoms and is picked up on a routine complete blood count. Some individuals with thrombocytopenia may experience external bleeding, such as nosebleeds or bleeding gum ...
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