Exenatide (Byetta)
1970-01-01 00:59:59
a synthetic version of a peptide (small protein) found in the saliva of the Gila monster (which is for some reason pronounced HEE-la), an intricately-patterned North American lizard capable of storing food in its tailis structurally similar to and so mimics the action of glucagon-like peptide 1 (GLP-1), an endogenous (made by the body) incretin (hormone made by the intestine that enhances the secretion of insulin after meals) that is important for regulation of glucose levels in the body and is deficient in diabetics enhances glucose-induced insulin release from beta cells in the pancreasused to treat type II diabetes (doesn't work on type I since people with this form generally have no beta cells, which is why they are diabetic in the first place)administered in combination with other anti-diabetic drugs (i.e. as an add-on or adjunctive therapy) to permit better control of glucose levels main side effects are nausea and vomitingMikhail N. Exenatide: a novel approach for treatment of
Safrole
1970-01-01 00:59:59
rhymes with arteriole, bronchiole, and vacuolealso known as shikimol or 5-allylbenzo-1,3-dioxolea colourless to slightly yellow (think the colour range of healthy pee) oily liquid at room temperatureextracted from the root bark of the sassafras tree and also present in low levels in numerous other plantshas been used as a flavouring agent in root beer (the original flavour), sassafras tea, and other foodsin 1960, the FDA banned its use in the USA as a food additive after is was found that it causes liver cancer in ratsno reported cases of liver toxicity or cancer in humans have been attributed to sassafras consumption - it is important to realize that not all substances that are carcinogenic in lab animals cause cancer in humans (i.e. animal models do not always predict the toxic effects of a substance in humans)is used in the synthesis of piperonyl butoxide (added to insecticides to increase their potency) and the mood-modifying amphetamines MDMA (Ecstacy) and MDE (Eve)http://en.wikip
Imiquimod
1970-01-01 00:59:59
trade name is Aldara (5% topical cream)topical immunomodulator (applied to and acts only on the superficial layers of the skin to modify the local immune response)used to treat external genital warts (oh great, another addition to my list of MEDICAL CONDITIONS I REALLY REALLY DON'T WANT TO GET EVER), actinic keratoses (a skin condition that often precedes the development of skin cancer), and superficial skin cancers (basal cell and squamous cell carcinomas and melanoma that appear as a red scaling patch on the skin)increases the production of cytokines (signalling molecules that are similar in function to hormones), which activate the immune system (both innate and adaptive immunity), thus increasing the ability of the body (specifically, the skin) to deal with viral infections and cancerous growthssince it has a relatively non-specific mechanism of action, it is likely also effective against other viral infections of the skin and superficial skin cancersmay soon find work as an anti-
Darbepoetin alfa (Aranesp)
1970-01-01 00:59:59
synthetic form of recombinant human erythropoietin (epoetin)erythropoietin is an glycoprotein (protein with a bunch of sugars attached to it) hormone produced mostly by the kidney that stimulates erythropoiesis (production of red blood cells by the bone marrow)epoetin and darbepoetin are manufactured using recombinant DNA technology:a gene encoding the protein/drug is inserted into a bunch of mammalian cells (usually Chinese Hamster Ovary cells)cells that begin to produce the drug are isolated and cultured in a bioreactor (placed in a controlled artificial environment and permitted to multiply)cultures of cells are processed to harvest the drug (see why they call it molecular farming?)the gene encoding epoetin is identical to that which is found in humans, but the gene encoding darbepoetin has been tinkered with such that darbepoetin contains more sialic acid (a type of sugar) groups than epoetin - this modification increases its half-life three-fold and enhances its activity relative
Q & A #2
1970-01-01 00:59:59
Yes, folks, it's that time again. That time when I scroll through the long list of search queries that brought people to this blog and pick out ones that were posed as questions that I would like to answer. Check out my first instalment of this fun little exercise here. As always, incorrect spelling and grammar have been subjected to the righteous fury of a semi-literate man. Myself.Can I use Tylenol to kill a cat ?Yes. But don't, because cats are nice and overdosing on Tylenol (acetaminophen) is a mean way to die, not to mention the fact that YOU'D BE KILLING A CAT. Jesus, if you really don't want it, drop it off at the local humane society or take it to a vet to get it put down. But don't do it yourself. By the way, cats are apparently highly sensitive to the hepatotoxic effects of acetaminophen, to the point that even a small portion of a single pill can do them in!What organs are affected by LSD ?LSD affects any tissues that express serotonin 5-HT2 receptors, since these are t
Protamines
1970-01-01 00:59:59
a group of nuclear proteins found in the sperm of many animalsmay have a role in the maturation of spermies and/or protect the genetic material (haploid chromosomal DNA, natch) that they carry - thus they may have a role in male infertility (i.e. if your protamines are mutated or expressed at abnormal levels, you're probably going to have to adopt)are used to make neutral protamine Hagedorn (NPH) insulin, an intermediate-acting form of insulin that is formulated such that when it is injected subcutaneously (under the skin) the insulin will be absorbed in a manner that closely resembles how it is normally released by the pancreas into the body AND it will last longer than regular old insulin and so reduces the number of daily injections required by diabeticsprotamine sulphate is used as an antidote to an overdose of heparin, specifically the uncontrolled bleeding that this entails, acting to bind heparin in a stable complex that blocks its anticoagulant activity - this effect is select
Heparin
1970-01-01 00:59:59
natural anticoagulant (stops blood from clotting) found primarily in liver, lung, and intestinecommercially extracted from the internal organs of cows and pigs (this enticing mix is also known as offal), although a recombinant (mass produced by bacteria) bioheparin is in developmentis the strongest organic acid present in the body (take that, uric acid!)can only be given by injection since it is broken down by the stomach and is poorly absorbed via the intestinefew side effects, the only big concern is hemorrhage (uncontrolled bleeding) from overdoseKalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
Toxins from mammals
1970-01-01 00:59:59
Snakes and frogs are obvious examples of animals that are capable of producing venom, which they tend to employ to capture prey and/or defend against predators. However, one does not generally associate mammals with being venomous (unless of course, one is a mammologist or is exceptionally good with trivia). Truly I say to you, several mammals, members of the order Insectivora, are actually venomous. These creatures produce toxins in their salivary glands that are secreted along with, and so present in, their saliva. They include the platypus, the Haitian solenodon (Solenodon paradoxus), and several species of shrew. In case you were wondering, shrews have five toes, while rodents have four.Blarina toxinThe venomous saliva of northern short-tailed shrew (Blarina brevicauda), which is native to North America and is roughly the size of a house mouse, is known to contain at least one toxic compound, blarina toxin (BLTX). This shrew is an insatiable little bugger, eating almost constantly
Q & A
1970-01-01 00:59:59
I use Google Analytics to track the people (including you, welcome reader!) who visit my blog. In addition to telling me how many people visit each day and where they are from and exactly what web browsing software they are utilizing (Firefox rules!), I get to see what keywords bring people to my blog. In other words, what they are typing into Google (or Yahoo or MSN Search or whatever) that gets them here. Occasionally these queries are stated as questions, some of which are inadvertently answered by the contents of this blog, others of which are not. Therefore, in the interest of keeping things mildly interesting (which is the only sort of interesting that I do) I am going to attempt to answer some of the more unique questions that have been posed. Please note that I've edited for spelling or grammar where necessary.Does catnip cause hangovers in cats ?Hmm. Well, catnip contains a psychedelic drug, and most psychedelic drugs that I have heard of will cause a mild hangover in some pe
Phosgene
1970-01-01 00:59:59
also called carbonyl chloride or CG (I'm partial to phosgene, myself)a colourless gas with a musty odour that was developed and employed as a chemical warfare agent during WWI, first being used by the German army in December of 1915was the most effective lethal chemical agent used in WWI, accounting for about 80% of the approximately 100,000 gas-induced casualtiesis also used in the manufacture of plastics and is produced as a by-product of welding and from the combustion of chlorine-containing household productsfollowing inhalation it is transported deep into the gas-exchanging region of the lungs, where it slowly reacts with water to produce hydrochloric acid and carbon dioxide - the acid causes tissue damage, leading to the development of pulmonary edema (accumulation of fluid in the lungs)is an alkylating agent and so is carcinogenicacute exposure presents as eye, skin, pulmonary, and gastrointestinal irritation, with pulmonary edema often developing as a delayed symptom preceded
Valacyclovir
1970-01-01 00:59:59
also known to those who hate the letter 'y' (I know you're listening, Britain!) as valaciclovirtrade name is Valtrex (see: Paris Hilton)is a prodrug, meaning that it is converted into acyclovir, the drug that actually does drug stuff, once it is absorbed into the bodyis active against both types of the herpes simplex virus (both can cause blistering of the mouth and/or genitals) and the varicella zoster virus (VZV, causes chickenpox when you first get infected with it, then it goes into hiding and is reactivated in some people in later life to produce herpes zoster, or shingles)doesn't curve these viral infections (there is no cure...mwahahahaha) but can reduce duration of symptoms and promote healingis a nucleoside analog, meaning that it mimics the basic components of DNA and RNA in order to mess with the replication and spread of the aforementioned viruses
Hirudin
1970-01-01 00:59:59
potent polypeptide anticoagulant derived from the saliva of the blood-sucking leech Hirudo medicinalisuse of this leech for medicinal purposes dates back to ancient Egyptleech application has been used in reconstructive microsurgery to alleviate venous congestion (pooling of blood in veins) in flaps and free pieces of tissue (read: partially torn or completely cut off fingers, ears, lips, nasal tips, etc.) that are being reattached, improving their survivalinhibits thrombin, the central enzyme responsible for controlling the coagulation process (clotting of blood), by binding to it at a site separate from it's active site (the site where it does it's enzyme stuff) and then covering the active site over - is the most potent known natural thrombin inhibitor and one of the most potent natural anticoagulantsfirst isolated and named in 1884, but it's structure and mechanism of action weren't discovered until 1955lepirudin and desirudin are recombinant (see this post) forms of hirudin pr
Nepetalactone
1970-01-01 00:59:59
psychedelic drug present in catnip (Nepeta cataria) that causes cats to party hearty (sniffing, rolling around, rubbing their chin against things, etc.)unusual since most psychotropic drugs (those that act on the brain) affect a wide variety of mammalian species (this drug only appreciably affects cats)only works by inhalation, feeding cats the plant in an encapsulated form (as a pill) produces no effectis a terpenoid, a class of aromatic (as in they have a scent, not a benzene ring) chemicals that include menthol, camphor and the cannabinoids (THC baby!)insect repellant and aphid sex pheromone (besides the inherent awesomeness of this, it also enables the drug to be used to spread aphid diseases as an alternative to using insecticides)Perrine, Daniel M. The chemistry of mind-altering drugs: history, pharmacology, and cultural context. Washington, DC: American Chemical Society, 1996.
Sildenafil (Viagra)
1970-01-01 00:59:59
inhibits PDE5, an enzyme that breaks down cGMP (a signal molecule that, in this case, controls blood flow) in the corpus cavernosum (a spongy region of expandable erectile tissue found along the length of the penis), with the resulting increase in cGMP causing vasodilation (expansion of blood vessels due to the relaxation of smooth muscle in their walls) leading to increased blood flow into the penis and the production of a boner (yeah, after all that I totally said boner)in individuals with normal erectile function, cGMP is increased by the release of nitric oxide (NO) from nerves in the corpus cavernosum when you get horny or during REM sleep - NO is a gas that can bind to and stimulate guanylate cyclase, an enzyme that produces cGMPfun side effects: sneezing, priapism (perma-boner, it stays up for longer than four hours), photophobia (you become crazy sensitive to light), visual changes (blurring, bluish tinge, loss of peripheral vision)Kalant H, Grant D, and Mitchell J. Principles
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Vancomycin (Vancocin)
1970-01-01 00:59:59
antibiotic (drug that kills or inhibits the growth of bacteria) capable of dropping a world of hurt on bacterial cell wall formation (most bacteria need a cell wall surrounding them to survive)unlike most drugs, which are rather small (250-450 Da), this is a biggie (~1500 Da) made up of sugars and amino acidsisolated from a bacterium found in soil from Indonesia and India (many bacteria are capable of harming/killing other bacteria in order to compete for resources)can cause a "red man" syndrome featuring flushing and a rash if given intravenously (via a needle into your vein) - is likely the result of excessive histamine (the stuff that makes you feel yucky when you get allergies such as hay fever) releaseKalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
Precious medicines: Platinum, gold, and silver as therapeutic agents
1970-01-01 00:59:59
It's true. Precious metals are used as drugs. As a complete and utter pharmacology nerd, I happen to think that this is awesome. Let me tell you some things.Platinum
Platinum-containing compounds represent an important class of anticancer / antitumour / antineoplastic agents, the prototype of which is cisplatin (Platinol). Cisplatin was first synthesized in 1844, but it was not until 1965 that it's ability to inhibit cell division was discovered. Like the discovery of penicillin, it was made totally by accident.A dude named Barnett Rosenberg was delivering electric current to cultures of bacteria as part of a series of experiments that he was doing. Rosenberg made the observation that the ability of the bacteria to multiply was inhibited in these cultures. It was soon realized that the inhibition of bacterial growth was due to the presence of platinum coordination complexes, among them cisplatin, in the cultures. These complexes were being generated by the platinum electrodes that wer
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Bismuth Subsalicylate
1970-01-01 00:59:59
the active ingredient in Pepto-Bismol (or if you're a cheapo university student like me, Life brand Stomach Ache Settler) and Kaopectateis a salt consisting of bismuth (a cool-looking heavy metal) and salicylic acid (essentially the same drug found in aspirin)causes the best harmless side effect ever: temporary darkening of the tongue and/or stool (read: black poo!)purported to be an excellent hangover cure, which makes sense given its stomach-settling propertiesthe crazy thing here is that salicylic acid, when taken chronically, can cause peptic ulcers, while bismuth salicylate, which contains salicylic acid, can be used to prevent and treat such ulcers (by coating the lining of the stomach to help protect it from digestive juices)http://en.wikipedia.org/wiki/Bismuth_subsalicylate
Loperamide
1970-01-01 00:59:59
trade names include Lopex, Imodium, and Dimoranalogue of meperidine (a synthetic opioid) used to deal with diarrhea / suppress the squirts / prevent the poops / revert the runs / thwart the trots / squash the skittersacts on opioid receptors in the gastrointestinal tract to decrease fluid secretion and peristalsisalso used to treat fecal incontinence (loss of the ability to restrain from pooping) since it increases anal sphincter toneis metabolized in the intestinal wall, so very little of it is absorbed into the circulation and delivered to the rest of the bodybecause it is mostly charged at physiological pH, it cannot cross readily into the brain, so even though it is an opioid like morphine or heroin it cannot get you stoned and so has no potential for causing dependence like those drugs
Lithium
1970-01-01 00:59:59
a soft, silver white metal used to make batteries for electronicsthe drug is actually a lithium saltmood stabilizer, meaning that it can be used to treat both mania (super happy) and depression (super sad), which makes it handy for treating bipolar disorder (which features alternating episodes of mania and depression)won't really do anything to healthy people (who are already mood stabilized)annoyingly unclear mechanism of action, something to do with altering adenylyl cyclase and phosphoinositide signal transduction pathways (yeah, i have no idea)Kalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
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Arecoline
1970-01-01 00:59:59
found in the betel nut (chewed in many Asian countries as a pick-me-up)thought to be responsible for addiction to chewing the nuts (haha nut chewing) due to its nicotine-like effects on the brain (nicotine being the addictive substance in tobacco)no medical use (haha nut chewing)Kalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
Ibogaine
1970-01-01 00:59:59
long-acting (~10 hours) psychedelic drug found in the root bark of Tabernanthe iboga, a shurb/tree/moderately-sized plant that grows in western Africaanimal research suggests that it acts via the same mechanisms as LSD, MDMA (Ecstasy), and some opioidsclaimed to be a cure for drug addiction and alcoholism by a former heroin addict named Howard Lotsof (research is currently ongoing, though if it doesn't pan out it may be necessary for Mr. Lotsof to change his name to Mr. Fullof)has been found to significantly reduce alcohol consumption in alcoholic ratsresearchers at Johns Hopkins (a very fine American university) found that, at high doses, it destroys part of the rat brain that may have a role in addiction, suggesting that while it might cure addiction, it also might eat away at your brainPerrine, Daniel M. The chemistry of mind-altering drugs: history, pharmacology, and cultural context. Washington, DC: American Chemical Society, 1996.http://en.wikipedia.org/wiki/Tabernanthe_iboga
Delta-9-tetrahydrocannabinol (THC)
1970-01-01 00:59:59
When I started this blog, way back in November of 2006, I made it my priority to post in a vague and interesting manner about drugs and poisons that the average person would probably know little to nothing about. However, the time has come, good reader, for my coverage of one of the big boys of the drug and poison world. Based on the queries that you have been making using that search box over yonder, I figured it was 'high' time that I discuss the drug we've all been waiting for... delta-9-tetrahydrocannabinol, or THC, as you kids like to call it.Now, I don't want to have to 'hash' out every last detail for y'all, so I'm gonna cover the basics, tell you to click here or here for more information, and then try to tell you something you didn't already know about THC. Given the subject matter, I felt that it was appropriate to discard my detached, sarcastic, and yet infinitely lovable persona and try to explain THC to you through the red eyes and giggle-injected ramblings of a t
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Teh Rejects: Drugs that didn't make the cut
1970-01-01 00:59:59
When a drug is first isolated/synthesized and preliminarily investigated by a pharmaceutical company for possible development into a marketable drug, it is often assigned a code number for use by the company. If the drug is then found to be capable of producing a useful pharmacological effect (e.g. reducing blood pressure) without serious toxicity (e.g. liver failure) in animals, it is given a catchier name (like ibuprofen or bacitracin) and evaluated in humans in a series of clinical trials. Should these trials confirm the animal results, and the drug is more effective than currently available drugs that do the same thing (if these drugs are available), and the government is happy with the way things were carried out, a new drug can be brought to market. Hooray!The majority of drugs that are developed by drug companies never make it to market. A good number of them don't even make it to human trials, and thus are never even granted a nifty moniker. Instead, they retain a boring old d
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Meperidine (Demerol)
1970-01-01 00:59:59
is an opioid analgesic (morphine-like painkiller)it doesn't shrink your pupils (miosis), a telltale sign of morphine or heroin or oxycodone addiction, so it is the drug of choice for junkie doctors and nurses who want to keep things on the DLunlike morphine or heroin, which are derived from the opium poppy (Papaver somniferum), this bad boy is synthesized from organic precursors, often petroleum-derived, via complicated chemical reactionsKalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
Camptothecin
1970-01-01 00:59:59
cancer-zapping agent discovered in the 1950s as an unexpected result of a research effort to find a cheap plant-derived source for cortisone synthesiscortisone was found to be a potent anti-inflammatory agent in the 1940s, creating a huge demand for itat the time, the only available source for cortisone was from animals, making it mega expensive (a single dose cost $1000 and required bile from 40 slaughtered oxes)eventually Mexican yams (genus Dioscorea) containing diosgenin, a plant steroid that could be converted into cortisone, were identified as an ideal source for inexpensive cortisone production - Mexico subsequently became the primary supplier of cortisone in the 1960spresent in the wood, bark, and fruit of Camptotheca acuminata, a deciduous tree found in southern China that has a long history of use in traditional Chinese medicineclinical trials (testing it on humans) in the early 1970s revealed that, although it wrecked terrible havoc upon tumours, it wrecked terrible havoc up
Teh Overdose: Drugs and poisons that you shouldn't kill yourself with
1970-01-01 00:59:59
Disclaimer: Yes, this post is pretty tasteless. However, it should be noted that I am in no way condoning suicide with this post. I am, in fact, merely pointing out why overdosing on the following compounds is a really bad idea.AcetaminophenAlso commonly known as paracetamol, APAP, and Tylenol, is the most common cause of intentional self-poisoning in adults since it is widely available and cheap. What doesn't appear to be well known is that at high doses this drug is selectively toxic to the liver. If you end up dying, it is only after spending several days in intense pain. This form of poisoning can be treated with N-acetylcysteine (NAC).ParaquatA bipyridylium herbicide found in many weed control products (e.g. Gramoxone), if ingested in sufficiently large quantities it will cause multisystem organ failure with death occurring within hours to a few days. However, should you fail to drink enough of it, it will selectively accumulate and persist in your lungs and slowly digest them wh
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Dimenhydrinate
1970-01-01 00:59:59
better known to car sickness aficionados as Dramamine or Gravolused to prevent or treat the nausea and emesis (barfing, puking, ralphing, spewing, vomiting, that sort of thing) associated with motion sickness, radiation sickness, being under general anaesthesia, chemotherapy, Ménière's disease, etc. is actually a combination preparation of two drugs: diphenhydramine (also known as Benadryl, an antihistamine that produces sedation and helps alleviate allergies, nausea and vomiting) and 8-chlorotheophylline (a derivative of theophylline, a relative of caffeine found in tea that is used to counteract the sedation of the first drug)in large doses can cause convulsions (young children are particularly susceptible), ataxia (loss of muscle coordination), stupor (just like it sounds), hallucinations (yes, people do abuse it to trip out...just spend the $5 on pot already!), coma, and respiratory depressionKalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto:
Salvinorins
1970-01-01 00:59:59
a group of related compounds present in the leaves of Salvia divinorum ('Mexican mint', 'magic mint'), a rare variety of sage that is used by the Mazatec Indians of Mexico for religious and medicinal purposes and only became known to western society in 1962the leaves or leaf extracts can be smoked to induce powerful hallucinations that last for a relatively brief period of timewhen smoked, you start feeling it about 30 seconds after taking a hit, peaks in 5-10 minutes, and then effects disappear over next 20-30 minutesonly salvinorins A and D through F are hallucinogenic, producing effects similar to those of LSDsalvinorin A is the best studied of these and has a potency similar to LSDunlike LSD, which acts via 5-HT2 receptors, these compounds are kappa opioid receptor agonists (there are three types of opioid receptors: mu, kappa, and delta - morphine is primarily a mu opioid receptor agonist)potential toxicity has not been fully investigated in lab animals or humans - so far no t
Caffeine
1970-01-01 00:59:59
Dudes and dudettes, I have many exams this week, so no posts for a while. Please check again next week for some, like, totally rad stuff!Edit: The completionist in me demands action, so here are some things about caffeine that you very possibly were not aware of:is a methylxanthine found in coffee - other methylxanthines include theophylline (in tea) and theobromine (in cocoa)inhibits phosphodiesterase and blocks the action of adenosine, thus making it easier for your muscles to contract (caffeine can cause muscle tissue to contract in vitro)is used to diagnose people who have a genetic predisposition to malignant hyperthermia, a condition invoked by general anaesthesia that causes your muscles to intensely contract, producing tonnes of heat such that you run an exceptionally high fever and the enzymes in your body begin to stop working and you die very quickly (can be treated with dantrolene, hyperthermia is also a side effect of ecstasy use)can be used to treat asthma, since it cause
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To barf, or not to barf: Drugs that control vomiting
1970-01-01 00:59:59
Your brain is almost entirely closed off from the rest of your body by a layer of tightly linked cells called the blood brain barrier (often abbreviated the BBB). Although nothing can pass between the cells of this layer, small and/or lipid-soluble chemicals such as water and THC are able to pass through the cells, and thus access your brain. There are a limited number of sites in the brain where the BBB is intentionally circumvented, for here lie neural structures that require access to the general circulation to carry out their functions.One of these sites is called the area postrema. It is a small tongue-shaped area that lies on the floor of the fourth ventricle in the brainstem, and is involved the co-ordination of emesis, or vomiting
. It is also called the chemical trigger zone (CTZ), which references its ability to stimulate other parts of the brain (the nucleus tractus solitarius and dorsal motor nucleus of the vagus - more info here) to cause you to puke if it detects a toxic s
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