Penicillin V - Stomach-friendly version of the classic bacteria killer

Folks, I'm sick again, this time with strep throat. I'm on antibiotics and the maximum amount of acetaminophen that one can take before one's liver is annihilated. So no blog posts for the next couple of days.

Edit: I'm all better now, so here is some information on penicillin V and it's bacteria-killing ways:

  • also called phenoxymethylpenicillin (I'm partial to penicillin V, myself)
  • is the basic form of penicillin that can be taken orally (e.g. as a pill) and be appreciably absorbed into the bloodstream and thus distributed throughout the body
  • penicillin G (benzylpenicillin) is a slightly different compound that must be given parenterally (by injection) since it is broken down by stomach acid - it is considered to be the definitive form of penicillin
  • generally the first-line (first choice) antibiotic used against infections caused by Streptococcus pyogenes (tonsillitis, pharyngitis or strep throat, certain skin infections)


Carcinogens I Have Known And Loved

Disclaimer: I have neither known nor loved these substances, but I like catchy post titles. So sue me.

Mustard gas

Bastard of a chemical. Let's say you get exposed to it. Great. Nothing happens right away. But then a couple of hours later these terrible blisters develop wherever the gas came in contact with your body. If it got in your eyes, you can go blind. If you breathed it in, it does a right number of your respiratory tract and can cause you to drown in your own body fluids (see: pulmonary edema). To top things off, it causes cancer. The only good thing I can say about it is this: it is responsible for the first anticancer drug. During WWII a stockpile of the gas was blown up (this happens in wars) in Italy, resulting in lots of people getting exposed to it. An interesting trend was noted, where those who were exposed to the gas had decreased white cell counts. Since Hodgkin's lymphoma (a type of cancer) was known to originate in lymphocytes (a type of white cell), researchers decided to see if they could use the gas to selectively kill the cancer cells (plus normal white cells, of course). They could, and the result was mechlorethamine (Mustargen), an analogue of mustard gas that ushered in the era of treating cancers directly with drugs. Two of the dudes who worked on this project, Louis Goodman and Alfred Gilman, went on to write a rad pharmacology textbook that is now the undisputed go-to resource for that wonderful field of science.

Heterocyclic amines

These bad boys (and girls) are primarily made when muscle meat (as opposed to organ meat) is cooked at high temperatures. We're talking frying, broiling, and barbecuing. Consumption of meats containing these chemicals has been linked to a number of cancers including stomach cancer, making it fairly likely that they are the cause. How does one go about minimizing exposure to these things, you ask. The key is to eat your stakes rare, microwave meats prior to cooking them (um...okay), and avoid gravy (the amines are concentrated in meat drippings, from which gravy is usually made).


Best known as the preservative agent in embalming fluid, this mofo has also found medical/scientific use as a disinfectant, a means of treating warts, and as a way of fixing tissues or cells so that they can be looked at under a microscope. It has plenty of industrial uses as well. It permanently attaches proteins with each other and with DNA, damaging or killing cells (if they are alive) and preventing tissues from liquifying, thus permitting open caskets to be a reasonably tolerable affair. Aside from the whole, you know, person being dead and stuff. Since it can damage DNA, exposure to high levels of this compound over a long period of time, which usually occurs via the inhalation of fumes (see: sawmill workers, undertakers, lab workers), increases your risk of developing nasopharyngeal cancer. Drinking formaldehyde is a bad idea. The body converts it to formic acid, resulting in fun things like metabolic acidosis, blindness (the enzyme that makes formic acid is highly expressed in the retina), coma, and even death. It's worth nothing that methanol (wood alcohol) is converted to formaldehyde by your liver, and thus produces a similar symptomatology (yay, big word!) if you ingest it.

Hexavalent chromium

Oh, hexavalent chromium. Why must you damage DNA so? Pop culture reference point for my non-science peeps: Erin Brockovich. Inhalation of particulate matter formed from compounds that contain this form of chromium increases your chances of getting the lung cancer. Regardless of the route of exposure, the lungs are often affected because they contain a zillion tiny capillaries in which particles containing the metal can become lodged. It is reduced in the body (i.e. electrons are added to it) to pentavalent chromium (also carcinogenic), and then to trivalent chromium. Pentavalent chromium can be oxidized back to the hexavalent form, and it is thought that this process generates radical oxygen species (ROS), namely hydroxyl radicals, which can damage DNA, leading to mutations and possibly cancer.



Gendicine - A drug of the future

Short one today, folks. I need to sleep. Don't think that I've failed anything so far.

  • recombinant adenovirus-p53 gene (gene therapy!) used to treat head and neck squamous cell carcinoma
    • essentially an adenovirus that has been engineered to carry a human p53 gene such that it will infect tumour cells and insert the gene into their genome, causing them to produce p53 and thus activate death mechanisms that make 'em kill themselves
  • currently approved for use in China, with similar drugs in development in other countries including the US of A
  • pretty frickin' cool
Patil SD, Rhodes DG, Burgess DJ. DNA-based therapeutics and DNA delivery systems: a comprehensive review. AAPS J. 2005 Apr 8;7(1):E61-77.



A short-acting barbiturate also known as sodium thiopental, Sodium Pentothal (Abbott Laboratories discovered it and trademarked it as this), thiopentone sodium, and trapanal. Your liver metabolizes it to pentobarbital, another short-acting barbiturate.

Good Thiopental:

Used by anethesiologists for the intial patient K.O., however, in small doses it wears off quickly (5-10 minutes), so long-acting inhaled anesthetics are used to keep the patients under. Has a long half-life (5-24 hours), so if it were the only anesthetic used, the patient'd be out for a long time, this varies by how much fat a person has because thiopental is redistributed to adipocytes. So the fatter one is, the longer the effect of thiopental would last (Big Mac meet
unconsciousness, unconsciousness, Big Mac).

Can be used to induce medical comas in cases of intracranial bleeding, during which your brain swells, from becoming squishier (a very bad thing), and also reduces pressure by reducing the activity of neurons, and thus the osmotic exchange rate.

Bad Thiopental:

Used in some...alleged...situations to inhibit higher brain function in hopes of getting people to tell the truth. This is based on the assumption that lying is more complicated than telling the
truth, which psychiatrists and kids who steal cookies before dinner hotly dispute.

Infamous for its role in the deaths of some of the wounded of Pearl Harbor. Traumatized or severely wounded personnel were given large doses of thiopental that proved to be too large.

Evil Thiopental:

Used as the initial drug in lethal injection to induce coma and make for painless state-sanctioned execution (in 37 states near you), along with pancuronium bromide and potassium chloride. Theoretically, thiopental alone could do the job, but that would take too long and Americans just don't have that kind of attention span.

Note: Today's post is brought to you by Toaster Sunshine, a faithful D&P reader with a knack for science blogging. Check out Toaster's blog at http://bioanthro.blogspot.com



Hi everyone. I've got a couple of exams this week, so I'm putting D&P on the backburner for a few days. Not to worry, I shall return!

P.s. Now would be a really great time for people to send me guest posts (drugsandpoisons [at] gmail [dot] com)


Thiabendazole (Mintezol, TBZ)

Hey there. Let me break it down for you, nice and easy like:


  • fungi (molds and spots and rots and blights) that spoil fruits and vegetables
    • messes up cell division, protein synthesis, and cellular respiration
    • sprayed on crops and used as a food preservative
  • parasitic worms that cause disease in livestock and humans
    • messes up cellular respiration (citric acid cycle) by inhibiting some enzyme
  • people poisoned with metals (lead, mercury, antimony)
    • it is a chelating agent that can bind said metals and facilitate their excretion from the body, thus limiting their toxicity


Trippin' in your own backyard: Psychedelic drugs in plants and fungi found naturally in the USA

First off, apologies in advance for the exclusive focus on the United States in this post. I realize that many of you aren't from the US of A. Heck, I'm not. But I found a cool article on PubMed and I thought you people might find it interesting. So I've summarized it for y'all. Don't know about you, but I have a tendency to associate drug-containing plants and fungi with exotic locales. Anticancer drugs from the Amazon Rainforest. Opium from Afghanistan. Cocaine from Columbia. That sort of thing. So when I came across an article on drugs, psychedelic drugs no less, found in plants and fungi that have established themselves in American soil, I was intrigued. Please note that I will be discussing species that are growing wild, not those being cultivated in greenhouses and suburban basements.

Phalaris aquatica
The short-acting hallucinogen DMT, most often associated with the Amazonian brew ayahuasca, is also present in appreciable quantities in several common species of grass belonging to the genus Phalaris, including P. aquatica (bulbous canarygrass, Harding Grass), P. arundinacea (reed canary grass), and P. brachystachys (shortspike canarygrass). These grasses can be found hanging out in the fields, sidewalk cracks, abandoned parking lots, and poorly-maintained lawns of Middle America. DMT is also found in the root bark of Desmanthus illinoensis (prairie bundleflower), which is also found throughout the Land of Liberty.

Psilocybe subaeruginascens
Psilocybin is one of several related hallucinogens found in a number of mushrooms belonging to a number of genera, including Gymnopilus, Panaeolus, and Psilocybe. While these 'magic mushrooms' are historically associated with Mexico, where they used religiously by the native peoples of Mesoamerica, many species are found growing on cow and horse poop in the USA. That's right folks, many shrooms are coprophagous (they grow on and consume feces). So the next time you eat some, try not to think about that. Bad trip. As far as localization goes, they are generally found along the coastlines of the Gulf of Mexico (Florida to Texas) and Pacific Northwest (including California).

In the desert along the Texas-Mexico border, you can find Lophophora williamsii (peyote). This spineless cactus is the natural source of mescaline, a hallucinogen enjoyed by luminaries such as Aldous Huxley and Eli Cash.

Lysergic acid amide (LSA), a natural analogue of LSD, is found in the seeds of of Argyreia nervosa (Hawaiian baby woodrose) and several members of the genus Ipomoea (morning glory). The woodrose is found only in Hawaii, having been introduced from Asia, while morning glory plants are found across the US. LSA is also present in Achnatherum robustum (aka Stipa robusta or Sleepy grass), which is found in the American southwest.

Datura Stramonium
In addition to the classic hallucinogens, there are a number of drugs capable of producing a toxic delirium that features hallucinations. These so-called dissociative agents are generally much more dangerous than the hallucinogens. Atropine and scopolamine, anticholinergic dissociative agents, are found in a number of plants belonging to the Solanaceae family that grow wild in the States. These include Datura stamonium (Jimson weed), Atropa belladonna (deadly nightshade), and Mandragora officinarum (mandrake), and Hyoscyamus niger (henbane). Of these, only plants of the genus Datura are native to the United States, the rest having being introduced due to their pretty flowers or something. Mushrooms of the genus Amanita, found throughout Canada's southern neighbour (ha, eat my Canadian spelling, suckas!), contain the dissociative agents ibotenic acid, muscimol, and muscazone. Unfortunately, some species also contain fun toxins like α-amanitin, which can cause lethal liver and kidney damage. These ones usually have scary names like death cap and destroying angel. Arguable the best known Amanita mushroom is Amanita muscaria, which looks pretty darn cool.

Halpern JH. Hallucinogens and dissociative agents naturally growing in the United States. Pharmacol Ther. 2004 May;102(2):131-8.


Carbonic anhydrase inhibitors - Fixing pretty much everything

  • class of drugs that inhibit (wait for it...) carbonic anhydrase (CA), an enzyme with a variety of functions specific to different parts of the body, enabling it to be used to treat a number of seemingly unrelated diseases
  • include acetazolamide (Diamox), methazolamide (Neptazane), topiramate (Topamax) and zonisamide (Zonegran)
  • are structurally related to sulfonamide antibiotics ('sulfa drugs'), from which they were developed
    • carbonic anhydrase inhibitors, thiazide diuretics and sulfonylurea antidiabetic drugs were all developed from sulfonamide antibiotics, after it was noticed that, in addition to killing bacteria, the antibiotics produced 'side effects' including diuresis, metabolic acidosis, and increased insulin secretion from the pancreas
  • things that these drugs can fix:
    • glaucoma - decrease the formation of aqueous humour, which reduces intraocular pressure
    • idiopathic (benign) intracranial hypertension - decrease the formation of cerebrospinal fluid (CSF), which reduces intracranial pressure
    • hypertension, congestive heart failure, cirrhosis with ascites - increase urine production (diuresis) so that you lose more fluid than normal, lowering blood volume and thus blood pressure (since PV=nRT, natch)
      • note: CA inhibitors are rarely used as diuretic agents since there are lots of other drugs capable of doing the same thing, only better
    • hyperkalemic periodic paralysis - increase urinary potassium excretion
      • note: can lead to mild hypokalemia (too little potassium in the blood) that can cause fun side effects like numbness and parageusia (things tastes weird)
    • mild altitude (mountain) sickness - increase urinary bicarbonate excretion, which increases the plasma concentration of hydrogen ion and thus relieves the effects of respiratory alkalosis that occur at high altitudes (the reduced availability of oxygen at higher altitudes stimulates respiratory centres in the brain resulting in increased ventilation, decreasing the plasma concentration of carbon dioxide and thus hydrogen ion)
    • cystinuria and hyperuricosuria - increase urinary bicarbonate excretion, alkalinizing urine so as to maintain acidic substances such as cystine and uric acid, which would normally precipitate out and form stones, in solution
    • epilepsy and migraine - increase cerebral blood flow and raise carbon dioxide levels in the brain, also block sodium channels and glutamate receptors and/or enhance GABA activity
Masereel B et al. Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. J Med Chem. 2002 Jan 17;45(2):312-20.


Aconitine - Numbs the pain, then breaks your heart

So yeah, aconitine is basically the annoying emo version of an alkaloid. Or something like that.

If one was so inclined as to do a fancy chemical extraction from the mashed up vegetative matter of any plant belonging to the genus Aconitum (otherwise known as aconite, monkshood, soldier's cap, helmet flower, or wolfsbane), one might be able to isolate a chemical called aconitine (along with a number of very similar alkaloids) capable of acting as both an analgesic (painkiller) and a cardiotoxin (causes arrhythmias, which are basically when your heartbeat gets thrown out of whack). Incidentally, the hood/cap/helmet name is the result of the characteristic helmet-shaped flowers that species of Aconitum produce. Also, wolfsbane sounds awesome (see also, the seemingly way less intimidating yet also very poisonous henbane).

Extracts of Aconitum species are used in traditional Chinese medicine to treat pain and inflammation. This is a great example of how natural/herbal remedies are often more dangerous than the drugs they attempt to replace. There's a damn good reason that aconitine has never caught on as a painkiller, and yet has occasionally been used to poison people.

Aconitine is thought to bind to and open voltage-dependent sodium channels in the heart and central nervous system, resulting in the disruption of electrical conduction in the heart (producing arrhythmias) and pain signals to the brain (producing analgesia) [1]. Because it has this particular mechanism of action, it is used to create animal models of cardiac arrhythmia, which help researchers to develop new antiarrhythmic agents [1].

[1] Gutser UT et al. (1998). Mode of antinociceptive and toxic action of alkaloids of Aconitum spec.. Naunyn Schmiedebergs Arch Pharmacol 357: 39-48.



  • monoterpene (like menthol or pulegone) that exists in two related forms, alpha and beta
  • present 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 absinthe
    • also 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 century
      • French 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 stuff
      • although popular with all levels of society, was especially revered by the artists (see: Degas, van Gogh, Picasso) and intellectuals (Verlaine, Wilde, Poe, Hemingway)
      • was banned throughout Europe and North America in the early 20th century due to it being linked (often erroneously) to all sorts of diseases including a syndrome called "absinthism" that featured hallucinations, blindness, convulsions, general nuttiness, and even death
    • besides absinthe, the major dietary source of thujone is actually sage and sage-containing products
  • has a chemical structure that is similar to tetrahydrocannabinol (THC) but it does not act on cannabinoid receptors
  • blocks GABA-A receptors, which normally keep the brain from becoming overactive by inhibiting neural activity, resulting in abnormal excitability (excitotoxicity) producing muscle spasms and convulsions
- Lachenmeier DW et al. Absinthe--a review. Crit Rev Food Sci Nutr. 2006;46(5):365-77.
- Rietjens IM et al. Molecular mechanisms of toxicity of important food-borne phytotoxins. Mol Nutr Food Res. 2005 Feb;49(2):131-58.



If only. R.I.P. Mr. Vonnegut.


Bremelanotide (PT-141)

  • 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 signaling erections (induces and facilitates erections) and increases activity in brain regions associated with sexual responses
  • doesn't appear to affect the vasculature of the genitals (like Viagra and co.) but instead appears to act directly on brain to increase sexual desire
- Diamond LE et al. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. J Sex Med. 2006 Jul;3(4):628-38.
- Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102.


Ethidium bromide (EtBr, homidium bromide)

  • 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 DNA
    • used as a stain to detect DNA as part of certain molecular biological techniques including microscopy and gel electrophoresis
  • is 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 transcription
  • is 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 teratogenic
  • also used to treat animal trypanosomiasis (parasites) since they bring the reaper down on these little nasties nice 'n well
Tettey JN et al. The effect of inducing agents on the metabolism of ethidium bromide by isolated rat hepatocytes. Chem Biol Interact. 1999 Nov 30;123(2):105-15.


Ziconotide (Prialt, SNX-111)

  • synthetic derivative of ω-conotoxin M-VII-A, a peptide toxin produced by Conus magus, a species of cone snail
  • used 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 depression
  • used 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 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 variety of voltage-gated calcium channel found primarily in neurons, disrupting calcium-dependent transmission of pain signals via the spinal cord to the brain
    • N-type calcium channel blockers (NCCBs) represent an exciting new class of neurological analgesic drugs
Klotz U. Ziconotide--a novel neuron-specific calcium channel blocker for the intrathecal treatment of severe chronic pain--a short review. Int J Clin Pharmacol Ther. 2006 Oct;44(10):478-83.


Fomivirsen (Vitravene)

  • 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 AIDS
    • CMV retinitis can progress to blindness, which sucks
    • CMV 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 harmless
  • is 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 required for viral replication and viral invasion of host cells and so these processes are disrupted by the drug
  • its unique mechanism of action makes it effective against varieties of CMV that are resistant to traditional antiviral drugs (traditional meaning drugs that aren't nucleic acids like ganciclovir and foscarnet)
Jason TL, Koropatnick J, Berg RW. Toxicology of antisense therapeutics. Toxicol Appl Pharmacol. 2004 Nov 15;201(1):66-83.


Isoniazid (isonicotinic acid hydrazide) - The original TB killer

  • first-line drug (literally, the first drug a doctor will turn to) for the treatment and prophylaxis (prevention) of tuberculosis
  • converted 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 resistance to chemical damage (including damage mediated by hydrophobic antibiotics) and dehydration
  • inactivated mainly by N-acetyltransferase, a liver enzyme that comes in two flavours - slow and fast - such that some people metabolize isoniazid more quickly than others (rapid acetylators vs. slow acetylators)
    • approximately 90% of Asians are rapid acetylators, while it's about 1:1 rapid and slow acetylators in Caucasians and Blacks
  • inhibits CYP 3A4, one of the major drug metabolizing enzymes in the body, resulting in elevated levels of other drugs being taken concurrently that are metabolized by this enzyme (this is a type of drug-drug interaction)
  • somehow causes the depletion of pyridoxine (vitamin B6) stores in the body, which can result in peripheral neuropathy, skin lesions, and anemia
- Kalant H, Grant D, and Mitchell J. Principles of Medical Pharmacology 7th ed. Toronto: Saunders Canada, 2006.
- Marcinkeviciene JA, Magliozzo RS, Blanchard JS. Purification and characterization of the Mycobacterium smegmatis catalase-peroxidase involved in isoniazid activation. J Biol Chem. 1995 Sep 22;270(38):22290-5.


Sucralfate (Carafate)

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 the gastrointestinal (GI) tract (specifically, the stomach or small intestine) by stomach acid, which is mostly hydrochloric acid that is secreted by specialized stomach cells called parietal cells. Normally the stomach is lined with mucus, which prevents the acid from eating up the stomach (ha, it's the stomach, get it?). However, in the event of things like chronic gastritis due to infection with Helicobacter pylori, psychological stress, chronic use of non-selective NSAIDs, smoking, and/or Zollinger-Ellison syndrome, either the mucus barrier is compromised or else the amount of acid being produced is abnormally increased, resulting in ulceration. The duodenum is the first section of the small intestine (there are three sections in total) that the stomach empties into. Incredibly, it is this part of the GI tract, not the stomach, that is the main site of peptic ulcer development.
When taken orally (by mouth), sucralfate travels to your tummy and does two things. Firstly, it binds up and neutralizes stomach acid, bile acids, and digestive enzymes. Secondly, it binds to proteins on the surface of ulcers to form complexes that cover and protect them from further exposure to stomach acid, bile acids, and digestive enzymes, thus preventing them from developing further and helping them to heal.



Resiniferatoxin (RTX)

  • analogue of capsaicin, the stuff in chili peppers (genus Capsicum) that makes them so friggin' hot
  • present 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 Islands
  • along 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 fibres
    • the initial excitation of these fibres is responsible for the burning sensation experienced with eating chili peppers and getting sprayed with pepper spray
    • by desensitizing the fibres, the transmission of pain is disrupted, producing an analgesic (painkilling) effect
    • RTX 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 the initial excitation (and pain) is negligible
  • effective means of increasing bladder capacity in individuals afflicted with neurogenic detrusor overactivity (NDO) of spinal origin
    • NDO is a condition featuring involuntary contractions of the detrusor muscle (the muscular coat of the bladder) while the bladder is filling with pee, causing you to feel like you have to pee a lot and piss yourself because you can't hold it
    • the desensitization of type C fibres that innervate the bladder depresses the activity of the muscle so that it doesn't contract as often
Silva C et al. Urodynamic effect of intravesical resiniferatoxin in patients with neurogenic detrusor overactivity of spinal origin: results of a double-blind randomized placebo-controlled trial. Eur Urol. 2005 Oct;48(4):650-5.