# Tag Info

17

The reason why the generic name of most drugs have seemingly little semblance to their chemistry is in the interests of practicality; a doctor would find it easier to write sildenafil (generic name) or Viagra (brand name) in a prescription than 5-{2-Ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-1-methyl-3-propyl-1$\ce{H}$,6$\ce{H}$,7$\ce{H}$-pyrazolo[4,...

14

Another reason is that many drugs which are conjugated to hydrochloride salts is they are amines, and amines by themselves often stink. So people might be turned off from taking drugs that smell terrible (fishy). Now, note that even though a label might say something such as "fexofenadine HCl" that doesn't mean there is HCl in the drug. Fexofenadine is an ...

13

Typically, a neutral drug species containing an amine nitrogen will have a higher melting hydrochloride salt that may be better than the "free base" in that it is easier to crystallize (and hence purify) for use in a drug formulation. But many types of salts are used besides the hydrochloride - it all depends on which salt gives good crystals and also works ...

10

In pharmaceutical industries, $56\%$ of the drugs currently in use are chiral molecules and $88\%$ of the last ones are marketed as racemates (or racemic mixtures), consisting of an equimolar mixture of two enantiomers. More recently, drugs originally marketed as racemic mixtures are reintroduced using the active isomer. Examples include racemic citalopram (...

10

One of the perhaps most important theory of anaesthesia is that: Most anaesthetics enhance the activity of inhibitory GABAa receptors and other cys-loop ligand-gated ion channels. Other important effects are the activation of a subfamily of potassium channels (the two-pore domain K+ channels) and inhibition of excitatory NMDA receptors Almost all ...

10

In short: no. It is not that simple. According to Wikipedia, atropine works as a muscarinic antagonist, which blocks the action of acetylcholine at the muscarinic acetylcholine receptor. So, the mode of action as an antidote is to prevent muscarine from binding to the receptor, thus inhibiting its effects on the body. The poisonous effects of atropine ...

9

It's the indole portion of the molecule. the lowest two rings...if you remove those, the compound has no such properties. Indoles, the side chains of tryptophan , an amino acid, are suitable for binding to receptors that affect emotion, perception, cognition, sleep/wake cycles etc. You can see how the indole looks similar to both DMT (dimethyltryptamine--...

9

Because amoxicillin is available as oral tablets, it can be ascertained that it is not significantly degraded to a useless form in the stomach. In fact, it has an oral bioavailability of 95% (meaning 95% of the orally ingested material goes into the blood stream rather than being destroyed in the stomach). The term for an oral medication being destroyed ...

9

The accepted answer is correct in some respects, though the assertion that an oral dose can be assumed to be safely crushed is only generally true. The Institute of Safe Medication Practices maintains a list of medications that can't be crushed (available for "free" on some sites, but with overlap in lists like this one). These medications are usually ...

8

The diethylamide "unit" dramatically potentiates lysergic acid. LS-Dimethylamide is significantly less potent, as are other/different amide or amine units. The differences in the amide or amine units also result in different experiences (spiritual, visual, auditory, etc.). Of course, it's different for everyone, but a loose analogy could be to the ...

8

According to several sources online the chemical weapon used in the failed assissination of Mashal was levofentanyl. This Wikipedia article states: On September 25, 1997, Mashal was injected in the ear with a toxin (thought to have been a derivative of the synthetic opiate Fentanyl called Levofentanyl). Another source reads: In September 1997, an ...

6

Question: When these foreign amines have been taken up into the vesicles how do they proceed?...Do they re-enter the synaptic cleft by exocytosis...How are they eventually cleared from the synaptic area? Here is the mode of action of these agents (indirectly acting sympathomimetics): The most important drugs in the indirectly acting sympathomimetic ...

6

I'm in a medicinal chemistry department, the floor below is the pharmaceutics department. We are both located in our university's college of pharmacy. The pharmacology department is under the college of medicine in same building as biochemistry, microbiology, etc. There is little interaction between departments here and that's not good. But we can break the ...

5

It's been suggested by Thomas Heimburg's group in Denmark (perhaps others) that anesthetics work by a common depression of the gel/fluid transition temperature in nervous membranes. Some virtues of this view include its consistency with the action of anesthetics being proportional to their partition in lipid (Meyer-Overton rule... and notice this rule ...

5

Here's a draft: First, read this paper. Considering we're under alkaline conditions (blood pH between 7.35-7.45) we'll take their alkaline mechanism proposal. Mechanism This is obviously incomplete, with good reason. Without knowing what the active site of the enzyme looks like (except for Ser70), it's difficult to devise of a mechanism. I could imagine ...

5

The naming of drugs is not completely a randomised process but depends on various factors most of which are linked to origins, chemistry or any modifications during the drug discovery pipeline although in old times serendipity discovery often led to trivial names being given to drugs. While morphine seems have been named arbitrarily, the same is not true ...

4

For a variety of explanations of industrial techniques as applied to acetylation, including acetaminophen synthesis, try here https://www.google.com/patents/US20120065423 The examples are right at the bottom and are only scaled down lab versions of the industrial technique. Over 90% yield should be easily achievable if acetic anhydride is used (and is ...

4

Rosuvastatin is metabolized to a limited extent by CYP2C9 to form an N-desmethyl metabolite and the other metabolite is the rosuvastatin lactone. The acid moeity (highlighted part) is likely to undergo glucuronidation first and subsequently lactonisation to form the rosuvastatin lactone Unlike other statins, rosuvastatin undergoes relatively little ...

3

Under physiological conditions, the counter-ion is almost entirely dissociated from the drug, meaning that the identity of the counter-ion isn't directly responsible for how well a drug performs. This has been looked at extensively by medicinal/formulation chemists, who often screen many salt forms looking for desirable properties. From the graph below, ...

3

They don’t. Drugs are molecules, and in spite of what homeopathy says, molecules have no brain, no desire and no memory. They will perform random motion depending on the corresponding Gibbs free energy. Therefore, the drug you swallow needs to be designed so that it either survives the stomach, duodenum, liver-produced enzymes, pancreas-produced enzymes, ...

3

From this? You can't. You need more information. Examples: Do you know other drugs of this family? Which chemical features do they have in common? The interactions mediated by these features are likely important then. Do you know how the drug is supposed to function (you mention competitive inhibition)? What does the natural substrate look like, and what ...

3

In almost all respects, deuterium behaves like hydrogen, chemically. You can safely drink pure $\ce{D2O}$ in reasonable quantities (though not enough to replace more than ~25% of the $\ce{H2O}$ of the body). In fact, prokaryotes can continue to grow in ~100% deuterated media, albeit more slowly. It does prevent mitosis in eukaryotes in large quantities, ...

3

[Basic] Receptor: a molecule in a cell membrane that responds specifically to a neurotransmitter, hormone, antigen or other substance. Agonist: Substance which initiates a physiological response when combined with a receptor. Antagonist: Substance which inhibits the physiological response when combined with a receptor. Allosteric: Substance which alters the ...

3

After consulting with a professor, the answer seems obvious. The two negative charges repel each other when the free cyclodextrin molecule is in solution, resulting in an "open" conformation that has the carboxylate groups facing "out". The thioether chains interact with the rocuronium as it is drawn into the large open face of the molecule. As the ...

3

When designing a total synthesis of some pharmaceutical, it is much easier to do a racemic synthesis compared to a total synthesis for one enantionmer, although this is not always possible. In most cases the molecule must have the correct absolute configuration to work to the highest potential. An example of this is oseltamivir (Tamiflu), it has 3 chiral ...

3

Very interesting question. I always thought that most of the hallucinogens would somehow act as agonists for serotonine receptors in the frontal cortex and thus trigger visual enhancements, but i've never been so much into bio- and neurochemistry. Anyway, I just found Psychedelics and the Human Receptorome at PLOS ONE, which might be an interesting survey, ...

3

The fluorocarbons that you mentioned do have polarized $\ce{C-F}$ bonds, but no ionic bonds. If you think ionic, think salts. I'm not a pharmacologist, but what about the local anestethics used at the dentist? Lidocaine (1), mepivacaine (2), and articaine (3) are frequently used. All these compounds have tertiary and secondary amino groups. (I've marked ...

3

NMR could likely be used to characterize a bulk sample of the drug and identify the presence of cysteine residue oxidation products, but would not be of much use for establishing that cancer cells oxidize (inactivate) the drug, nor precisely how it was inactivated, given the tiny amounts of material involved. Maybe LC-MS could be used. Probably worth pulling ...

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