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Clomifene (Clomid, Serophene, Milophene) 1970-01-01 00:59:59 what "fertility pills" are usually made ofused to treat female infertility due to anovulation (lack of ovulation)doesn't work if infertility is caused by the dude (defective or lack of spermies) or woman's infertility is caused by ovarian dysfunctioninhibits the negative feedback action of estrogen in the anterior pituitary gland, resulting in increased release of follicle-stimulating hormone (FSH) - this leads to a higher rate of ovulation and hence increased potential for pregnancycan actually cause multiple ovulation, increasing the risk of multiple birthssometimes four or five ova are released and fertilized - say hello to the local news crew, quintuplets!actually is a mixture of two geometric isomers, enclomifene and zuclomifeneused (abused?) by some male bodybuilders to block the estrogen-like effects (e.g. man titties!) produced by anabolic steroids and restore the body's natural production of testosterone (which is lost with steroid use)http://en.wikipedia.org/wiki/Clomiphen
Coprine 1970-01-01 00:59:59 a rare amino acid (derivative of glutamic acid) present in several edible species of mushroom belonging to the genus Coprinus ("inky caps") including the Common Inkcap (Coprinus atramentarius), a lawn mushroom that is, unexpectedly, fairly commonis thought that it or one of it's metabolites (cyclopropanone hydrate) inhibits the enzyme aldehyde dehydrogenase (ALDH)alcohol (ethanol) is primarily metabolized in the body by the enzyme alcohol dehydrogenase (ADH) into acetaldehyde, a fairly toxic substance responsible for many of the symptoms of a hangoveracetaldehyde is then further metabolized by ALDH into not nearly as toxic acetic acid, the stuff in vinegar that makes it taste and smell the way that it doesthe inhibition of ALDH results in the accumulation of acetaldehyde when alcohol is consumedgettin' smashed or even just having a single drink up to 72 hours after eating mushrooms containing coprine will cause acetaldehyde poisoning, symptoms of which include flushing of face and ne
Pulegone 1970-01-01 00:59:59 monoterpene present in essential oils from plants of the Lamiaceae (mint) familyparticularly high levels are found in the European (Mentha pulegium) and American (Hedeoma pulegioides) varieties of pennyroyalhas an odour similar to peppermint and camphorused as a flavouring agent, an ingredient in perfumes, and a flea repellentpennyroyal tea (and oil) is/was used in traditional folk medicine to promote menstruation and as an abortifacient to initiate self-abortionthere is a crappy Nirvana song about this (bring it, haters!)there is no scientific evidence available to support its efficacy in this regard (read: don't do this, it is a fantastically terrible idea!)ingestion of high doses of pennyroyal oil has been reported to cause organ toxicity - liver, central nervous system (convulsions), kidney, lung - and deathpulegone and one of its metabolites (menthofuran) are both bioactivated by liver enzymes to reactive oxidative intermediates that bind to cell proteins and cause liver damageAn
Galanthamine (Razadyne, Reminyl, Nivalin) 1970-01-01 00:59:59 reversible competitive inhibitor of acetylcholinesterase and allosteric modulator of nicotinic acetylcholinergic receptorsenhances brain function by increasing the amount of acetylcholine, a chemical substance required for the function of certain neural pathways, in the brainused to treat mild to moderate Alzheimer's diseasefound in several members of the Amaryllidaceae, a family of flowering plants that grow from bulbs and often produce nice-looking flowers (e.g. common snowdrop, one of the first flowers to bloom in the spring)originally used to treat poliomyelitis (polio), myasthenia gravis (a disease featuring progressive fatigue and muscle weakness), and muscular dystrophy in Eastern Europe during the Cold WarHeinrich M, Lee Teoh H. Galanthamine from snowdrop--the development of a modern drug against Alzheimer's disease from local Caucasian knowledge. J Ethnopharmacol. 2004 Jun;92(2-3):147-62.http://en.wikipedia.org/wiki/Galanthamine
Nitisinone (Orfadin) 1970-01-01 00:59:59 used to treat hereditary tyrosinaemia type 1 (HT-1), a rare genetic disease caused by a deficiency in fumarylacetoacetase (FAH), an enzyme involved in the metabolism of tyrosinetyrosine is my very favourite amino acid, since the body uses it to make a number of important biological molecules including thyroid hormones, melanin, and catecholaminestyrosine metabolism consists of a series of steps, with FAH being in charge of the last oneFAH deficiency causes the buildup of tyrosine metabolites produced by prior metabolic steps, several of which happen to be toxic to cellssince FAH is highly expressed in liver cells, HT-1 usually presents as liver failure or chronic liver diseasedoes its thing by inhibiting 4-hydroxyphenyl pyruvate dehydrogenase (HPPD), an enzyme with an annoyingly long name that is responsible for an early step in tyrosine metabolism (upstream of FAH), thus preventing toxic tyrosine metabolite productioninitially developed as a maize herbicide is a derivative of leptospe
Dehydroepiandrosterone (DHEA) 2007-03-02 21:28:00 steroid hormone made primarily by the adrenal gland that is also used as a drugthe adrenal gland can be thought of as a pair of triangular-shaped lemons (work with me, people) that sit on top of the kidneys - the rind (cortex) produces steroid hormones and the pulp (medulla) produces catecholamines (e.g. adrenaline)used by the body to make both androgens (e.g. testosterone) and estrogens (male and female sex hormones, respectively)cheating athletes, take note:in women, taking DHEA as a drug increases testosterone in women, leading to insulin resistance, acne, and masculinizing effects (kinda turns you into a dude - baldness, facial hair and increased body hair, lowering of voice, etc.)taking DHEA as a drug has not been shown to enhance gains in muscle size or strength produced with strength training alone and thus has little or no benefit for use in athleticsclassified as an anabolic steroid in 2004 in the US of A, making it a controlled substancepreviously was sold legally as a nutrit
Oseltamivir 2007-03-05 15:41:00 Ladies and gents, I have acquired for my own personal use a flu bug. Posts will resume when I can get out of bed. Cheers.
Myristicin and Elemicin 2007-03-08 04:14:00 found in nutmeg and mace, two common spices that are produced from the seed and aril, respectively, of Myristica fragrans, a nice lookin' tree with green leaves that is native to tropical southeast Asia and Australasiaare responsible for the psychedelic action of these spicesabout 1-2 teaspoons of spice can really mess you up: euphoria, visual hallucinations, psychosis, and feelings of impending doom and unreality PLUS impressively potent nausea, vomiting, and tremors (and lots of other stuff)nutmeg was at one point used therapeutically at doses of nine teaspoonfuls daily to control diarrhea associated with thyroid cancermakes sense since both compounds structurally resemble mescalineapparently myristicin is a moderately effective antibacterial agent, which would potentially make it a useful natural preservativeNarasimhan B, Dhake AS. Antibacterial principles from Myristica fragrans seeds. J Med Food. 2006 Fall;9(3):395-9.
Sodium fluoroacetate 2007-03-12 05:15:00 other, much cooler name: Compound 1080naturally occurring poison found in a number of plants from around the worldconverted in the body to to fluorocitrate, which disrupts the citric acid cycle, thus impairing cellular respirationthis is very badsince it messes up an essential metabolic component, there is no known antidote and few people survive significant ingestion of this substancediscovered by the Germans during World War IIthey were looking for new chemical warfare agentshighly potent (0.1 g can theoretically kill a man) but requires ingestion or injection to be effective, so not quite what they were looking for (inhalation is where it's at!)independently discovered by the Americans during the war and was introduced as a rodenticide (kills...rodents) in the US in 1946currently is used by farmers to kill various crop- and livestock-eating mammalsis also highly toxic to birds and insectsProudfoot AT, Bradberry SM, Vale JA. Sodium
fluoroacetate poisoning. Toxicol Rev. 2006;25(4):21
Flunitrazepam (Rohypnol, roofies) 2007-03-12 22:38:00 fast-acting and powerful sedative/hypnotic drug used primarily to treat insomnia and settle people down prior to giving them general anaesthesiais a benzodiazepine, meaning that it acts on GABA-A receptors, which are prevalent throughout the brain, to enhance the flow of chloride ions into neurons, resulting in a generalized depression of neural activity that results in sedation (feeling dopey) progressing to hypnosis (sleep)is about 7-10 times more potent than diazepam (Valium), the archetypal benzodiazepineall benzos also work as anxiolytic and anticonvulsant agents, as well as skeletal muscle relaxantswidely used recreationally to enhance the effects of alcohol and other drugs, although some people get high off of it alone (mechanism is unknown) or use it as a 'downer' to deal with the side effects of stimulants ('uppers')has been used as a date rape drug and to facilitate robberies (it causes anterograde amnesia in addition to sedation, so the victim often remembers nothing) an
Gadolinium 2007-03-14 19:34:00 a malleable and ductile rare earth metal named after Johan Gadolin, a Finnish scientist who discovered the best named element of all time, yttriumapparently discovering one element means you get another one named after you, what the deal?is strongly magnetic at room temperature and demonstrates a magnetocaloric effect (which means, of course, magnetic refrigerators!)motexafin gadolinium is a novel anticancer agent that enhances the ability of radiation therapy to kill cancer cellsconsists of a gadolinium cation contained in the centre of a large heterocyclic organic ring, much like a porphyrin ringseveral mechanisms of action, including acting selectively on cancer cells to deplete their stores of metabolites that they need to repair the oxidative damage caused by irradiationis currently being studied for use alone or in conjunction with radiation therapy in a number of different cancers, including those of the brain, lungs, kidneys, and pancreassolutions of organic gadolinium complexe
Benzylpiperazine (BZP) 2007-03-12 23:13:00 methamphetamine-like stimulant that has recently been the subject of much investigation in New Zealand (where it is legal and used as a party drug)effects include euphoria, enhanced sensory perception (whoa, this glo stick won't stop blinking out coded messages and this trance music tastes like the ocean!), hyperactivity, and stereotypy (constant repetition of certain meaningless gestures or movements, often seen in schizophrenics)repeated use leads to sensitization (less drug required to produce same effect) and cross-sensitization to crystal meth in ratsless potent and probably less addictive than crystal meth (but potentially addictive nonetheless!)several contributing mechanisms of action, with the net result being the enhancement of the effects of serotonin, dopamine, and norepinephrine (all monoamine neurotransmitters) in the brainwas originally designed in a lab to be an anthelmintic (works against parasitic worms) agent, to be used to expel wormies (particularly roundworms and
Itchy, itchy, itchy: Antifungals and the treatment of yeast infections 2007-03-16 03:15:00 Being a dude, I thank my lucky stars on a daily basis that I am not prone to fungus-type infestations of my nether regions. Let's hear it for external genitalia! A woman's special area, like many other parts of the human body, is inhabited by both bacteria and fungi. These microbes are usually just chilling out, growing slowly and not bringing any attention to themselves. A yeast infection occurs when Candida albicans, a yeast (which is a type of fungus), is given the opportunity to take over downstairs due to a change in the local environment, which can be caused by a number of things including antibiotics, pregnancy, and a weakened immune system. Candida sets up shop in the most holy of holies, and before you know it, you've got vaginal candidiasis (a yeast infection)! And just so you know, I plan to see how long I can go in this post without mentioning the actual anatomical terms for 'womanly bits'. I consider this to be an exercise in puritan restraint. And euphemisms are fun! Read more:yeast infections
Podophyllotoxin (Podofilox) 2007-03-21 22:08:00 non-alkaloid lignan toxin present in podophyllin, resin produced by the rhizomes of plants belonging to the genus Podophyllum, for which it and the aforementioned resin are named, as well as a number of other genera that I don't feel like listing since I'm pretty sure most of you don't care that much and I really, really want to avoiding bogging down my posts with boring information and hideously long-winded sentencesplants containing lignans are commonly found in traditional medicine, making them interesting starting points for the development of new drugsthe genus Podophyllum includes Podophyllum peltatum (American Mayapple), a perennial herb native to eastern North America that grows in coloniesis used as a topic antiviral agent in the treatment of condyloma acuminatum (genital warts!) caused by human papilloma virus as well as other types of warts found on one's naughty bitshas also been used in the treatment of psoriasis vulgaris and rheumatoid arthritiskills cancer cells but
Chloral hydrate (Aquachloral, Somnos, Noctec) 2007-03-26 03:52:00 (surfing gossip sites to avoid studying anatomy)..."Oh look, Mel Gibson went nutso again, turns out that Anna Nicole Smith overdosed on chloral hydrate, and Lindsay Lohan has a...WAIT, HOLD THE PHONE! A drug in the news (okay, admittedly the entertainment 'news') is a blog post in the making. Let's do this thing.oral sedative (calms you down) and hypnotic (puts you to sleep)one of the first synthetic drugs (made in a lab in 1832) and definitely the first synthetic CNS depressantrapidly converted by hepatocytes and erythrocytes into trichloroethanol, the active form of the drugwidely used up until the middle of the 20th century, after which it found limited use as a sedative, having been largely displaced by the barbiturates and benzodiazepinessince the 1990s it has been used primarily in pediatrics to sedate children prior to minor surgery as part of dental or diagnostic proceduresmoderately addictiveserious toxic effects of overdose include cardiac arrhythmias, cardiac and respirat
Lobeline 2007-03-31 01:03:00 stimulant found in flowering herbs (the best kind, if you get my drift) that belong to the genus Lobelianamed after Matthias L'Obel, a botanist and physician to William the Silent and James I (history!)Native Americans used Lobelia medicinally and as a substitute for tobaccoresembles nicotine in that it acts at nicotinic acetylcholine receptors in the brainis less active than nicotine at these receptors and so can diminish the stimulant effects of nicotinehas been used with modest success as a treatment to help people quit smokingdiminishes the stimulant effects of amphetamines since it inhibits their ability to increase dopamine levels in the braindopamine is a neurotransmitter thought to be responsible for the stimulant and reinforcing effects of amphetaminesmay block mu opioid receptors, which are what morphine binds to to produce its effectsMiller DK et al. Lobeline, a potential pharmacotherapy for drug addiction, binds to mu opioid receptors and diminishes the effects of opioid r
α-Latrotoxin 2006-12-18 21:18:00 neurotoxic (bad fer teh brain) protein present in the venom of widow spiders (members of the genus Latrodectus) including the infamous black widowone of seven latrotoxins, is the only one that is vertebrae-specific (only affects animals with a spine, so my chemistry prof should be safe! OH SNAP!), the others being primarily active against insects (the natural prey of the spiders) or crustaceansthe current theory is that four units of the protein can join together to form pores in cells, with the resulting changes in ion flux signalling the release of neurotransmitters from nerve cells, producing (among other things) muscle contraction, manifested as painful abdominal cramps and breathing difficultieshttp://en.wikipedia.org/wiki/Latrotoxinhttp://en.wikipedia.org/wiki/Latrodectism
(Ergoline derivatives) 2006-11-29 16:52:00 Okay, so we've all heard of LSD, right? Acid trips, Timothy Leary, "Tomorrow Never Knows", dirty hippies, "I am a golden god", etc. Fact is, LSD is but one of an impressively large number of derivatives of a compound called ergoline. These derivatives can be found in ergot (parasitic fungus that grows on grains and grasses), Hawaiian baby woodrose (climbing vine native to the Indian subcontinent but apparently also grown in Hawaii), and several species of morning glory (flowing plant that blooms in the morning). In addition to their use/abuse as psychedelic drugs, many natural and synthetic derivatives of ergoline have more legitimate applications:ergonovine and methylergonovine (Methergine, Methylergometrine) - directly stimulate contractions of uterine smooth muscle (oxytocic) - have historically been used to induce labour, but are now only used to prevent and treat postpartum and postabortion hemorrhage (uncontrolled bleeding occurring after birth or abortion) - contraction of the
Strychnine 2006-11-17 01:43:00 glycine receptor antagonist, meaning that it acts on the spinal cord and brain and messes with your ability to control the movements of your muscleshas a LD50 of 1 mg/kg, meaning that less than a teaspoon of it will kill you deadcauses violent convulsions (muscle spasms) with death resulting from either asphyxiation (being deprived of oxygen since you can't breath properly) or exhaustion (extreme fatigue due to the convulsions)present in several plants including the very obviously named strychnine tree (Strychnos nux vomica)in lower doses, enhances the ability of lab animals to learn how to navigate through a maze and to discriminate between different visual stimuli (i.e. it enhances their mental functions)http://en.wikipedia.org/wiki/Strychnine
Sucralfate (Carafate) 2007-04-02 19:57:00 In the drug blog business, it can get awfully tempting to just paraphrase Wikipedia articles all the time. I've done it on occasion, I will shamefully admit, but I usually try and get actual research articles as sources for my posts. And when I do succumb to my more basic urges (greed and laziness, if you must know) and 'rip off' the Wik, I just pick out a few choice tidbits, change 'em 'round and explain things differently so it isn't plagiarism, and then add some amusing little comments. It's not like I'm cutting and pasting. Anyway, I just had a lecture on gastrointestinal drugs, being a pharmacology student and all, and I thought this one in particular was pretty neat. Sucralfate is a sucrose sulfate-aluminum complex (a sugar with a bunch of metal salts attached to it) that is used to treat peptic ulcers, particularly those that arise in the duodenum, as well as gastroesophageal reflux disease (GERD). Peptic ulcers are essentially holes burned through the lining of th
Resiniferatoxin (RTX) 2007-04-01 20:36:00 analogue of capsaicin, the stuff in chili peppers (genus Capsicum) that makes them so friggin' hotpresent in high concentrations in the sap of the resin spurge (Euphorbia resinifera), a plant that looks very much like a cactus that is native to Morocco and the Canary Islandsalong with capsaicin, is able to excite and then desensitize type C afferent fibres (pain-transmitting pathways to the brain and spinal cord) by activating a particular type of calcium channel that is expressed selectively in these fibresthe initial excitation of these fibres is responsible for the burning sensation experienced with eating chili peppers and getting sprayed with pepper sprayby desensitizing the fibres, the transmission of pain is disrupted, producing an analgesic (painkilling) effectRTX is several thousands times more potent in desensitizing the fibres, making it a potential powerful analgesic agent (drugs based on RTX are currently in development) since it can be given in small enough doses that t
The ULTIMATE toxin list 2007-04-04 01:17:00 That's right. I've been working away at this little beauty, and it's time to share. It's still in early development, but hopefully it will soon grow into something that will make it worthy of it's namesake. Want to contribute? drugsandpoisons [at] gmail [dot] comCheck it out. Read more:toxin
Isoniazid (isonicotinic acid hydrazide, INH) 2007-04-04 18:15:00 first-line drug (literally, the first drug a doctor will turn to) for the treatment and prophylaxis (prevention) of tuberculosistuberculosis (TB) is a stubborn and deadly disease caused primarily by infection with the bacterium Mycobacterium tuberculosis (try and find it!)TB is widespread in the developing world, and still hanging around in the developed world due to the emergence of drug-resistant strains and increased susceptibility in many people due to immunosuppression by drugs (legal or otherwise) or infection with HIVconverted by a catalase-peroxidase (enzyme that functions primarily to rapidly detoxify hydrogen peroxide) to an active metabolite that inhibits the synthesis of mycolic acids, which are a major and unique component of the cell walls of mycobacteria (bacteria belonging to the genus Mycobacterium)mycolic acids provide mycobacteria with special cell walls that enable them to proliferate inside macrophages (and thus avoid the immune system) and increase their resistanc
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) 2007-01-03 01:44:00 thermal breakdown product of a meperidine-like synthetic opioid called 1-methyl-4-phenyl-4-propionoxypiperidine (MPPP) that is used by drug addicts as a heroin substitute and may be accidentally produced during the synthesis of MPPPproduces severe Parkinsonian symptoms in humans and primates (the humans are often addicts who unwillingly inject themselves with some MPTP-laced MPPP)hallucinations and near total immobility ('the frozen addict')is transformed in the brain to MPP+ (1-methyl-4-phenylpyridinium, in case you were wondering), which selectively destroys dopamine-releasing neurons in the substantia nigra, the area of the brain that is damaged in people with Parkinson's diseasein 1982, six people in San Jose, California were exposed to MPTP and developed Parkinson's disease - one of the docs who examined them wrote a book about his experiencesis used to generate a model for Parkinson's disease in lab animals, permitting the study of the disease and the development of ways to
Ziconotide (Prialt, SNX- 111) 2007-04-10 02:32:00 synthetic derivative of ω-conotoxin M-VII-A, a peptide toxin produced by Conus magus, a species of cone snailcone snails are way cool: they use a venomous harpoon to catch fish AND they have rad looking shellsused to alleviate severe chronic pain but is neither an opioid nor a NSAID, these being the two main classes of analgesics (painkillers)unlike opioids does not appear to be addictive (no tolerance or dependence) or cause respiratory depressionused only when all other possible therapy options have been exhausted, including injecting morphine directly into the spine, since it must be injected directly into the cerebrospinal fluid (CSF) within the spinal cord to work (this is pretty darn invasive and so kinda risky)can't be given orally since it is a peptide and so is broken down by the stomachcan't be given intravenously since it causes profound systemic side effects (it is derived from an incredibly badass toxin, after all!)does its thing by blocking N-type calcium channels, a v
Fomivirsen (Vitravene) 2007-04-09 03:03:00 antisense oligonucleotide (ASO) used specifically to treat retinitis (inflammation of the retina) caused by an infection with cytomegalovirus (CMV) in immunocompromised patients, particularly those with AIDSCMV retinitis can progress to blindness, which sucksCMV belongs to the same family as the viruses that cause chickenpox and herpes, and gets its name from the fact that it produces very large (-mega-) cells (cyto-)most people become infected with CMV at some point in their lives, and it then sticks around for the rest of their lives, but a normal functioning immune system can usually keep it down such that it remains harmlessis injected directly into the vitreous humour of the eye (awesome and gross at the same time!) by an ophthalmologist (eye surgeon, often one who has specialized in vitreoretinal surgery)reduces the levels of viral mRNA transcribed from certain immediate-early CMV genes, which in turn reduces the levels of the proteins that they encode these proteins are require
Bremelanotide (PT-141) 2007-04-11 18:55:00 synthetic peptide analog of alpha-melanocyte stimulating hormone (α-MSH) that is currently being developed as a treatment for sexual dysfunction, specifically erectile dysfunction and sexual arousal disorder (cue a spike in my search traffic, hooray for sexy keywords!)α-MSH is a peptide hormone that acts via melanocortin receptors to do interesting things like turn you on and cause your skin to produce more melanin (pigment)has been shown to cause a rapid dose-dependent increase in erectile activity in dudes and increase sexual arousal in both the ladies and the gents derived from melanotan-II (MT-II), a cyclic lactam analog of α-MSH that is being developed as a sunless tanning agent (it was during studies with this compound as a tanning agent that it's ability to cause erections was discovered, much the same way that Viagra was discovered, leading to the development of bremelanotide)stimulates certain neurons in rat brain (specifically: hypothalamus) that are responsible for sign
Ethidium bromide (EtBr, homidium bromide) 2007-04-11 02:24:00 fluorescent toxicant (toxic man-made chemical) widely used as a molecular probe because it interacts with DNA and fluoresces with increasing intensity when it binds to DNAused as a stain to detect DNA as part of certain molecular biological techniques including microscopy and gel electrophoresisis an intercalating agent, which means that it is capable of inserting itself between the paired stands of DNA, deforming it and potentially messing up important cellular processes like DNA replication and transcriptionis strongly mutagenic, as it causes frameshift mutations in several strains of Salmonella typhimurium, a species of yeast used to assay mutagenicity (see: the Ames test), when it is metabolically activated by CYP P450-dependent mixed-function oxidases (a class of liver enzymes that oxidize chemicals)this suggests that it may be carcinogenic and teratogenicalso used to treat animal trypanosomiasis (parasites) since they bring the reaper down on these little nasties nice 'n wellTet
Anti-Gerasone 2007-04-13 00:55:00 If only. R.I.P Mr. Vonnegut.
Thujone 2007-04-13 18:47:00 monoterpene (like menthol or pulegone) that exists in two related forms, alpha and betapresent in a number of plants, most notably grand wormwood (Artemisia absinthium), a shrub native to Europe, Asia, and northern Africa that is used to make absinthealso found in Salvia officinalis (sage), Salvia sclarea (clary), Tanacetum vulgaris (tansy) and members of the genus Juniperus (junipers)absinthe ("green fairy" or "fée verte" for my French-speaking readers) is a highly alcoholic (damn straight!) emerald-green spirit that was arguably the most popular spirit drink in Europe in the late 19th centuryFrench soldiers fighting in Algeria in the mid 19th century were given alcoholic drinks containing wormwood to protect them from infectious diseases and increase morale, leading to boom in the popularity of absinthe as they returned home having developed a taste for the stuffalthough popular with all levels of society, was especially revered by the artists (see: Degas, van Gogh, Picasso) and int
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