Pharmacology & Chemistry - what happens to the drug while in the body.

R4NS0M's picture
Posts: 2
Joined: 2008-10-15

Anyone who is interested in the chemistry side of some of the commonly discussed medications and side effects as well as half-life information, drug interactions, etc. etc. i thought that this would be a cool subject to place a starting point for some of the following topics. Discussion of questions, answers, opinions, experiences and any thoughts are all welcome and deemed to be fair game.

Most common subjects of discussion:

  • Pharmacokinetics
  • Absorption
  • Distribution
  • Metabolism
  • Elimination
  • Adverse Drug Effects
  • Toxicology
  • Drug interactions

Cool





R4NS0M's picture
Posts: 2
Joined: 2008-10-15
MAOI (Monoamine oxidase inhibitors) & Hypertensive Crisis Risks

<R4NS0M LIFE="EXPERIENCE" KNOWLEDGE="POWER" MYGOAL="SAFETY">

MAOI's and SAFETY

SELECTIVITY

MAOIs differ by their selectivity of the MAO receptor. Some MAOIs inhibit both MAO-A and MAO-B equally, other MAOIs have been developed to target one over the other. MAO-A inhibition reduces the breakdown of primarily serotonin, epinephrine, and norepinephrine and thus has a higher risk of serotonin syndrome and/or a hypertensive crisis.

  • MAO-A inhibition reduces the breakdown of primarily serotonin, epinephrine, and norepinephrine and thus has a higher risk of serotonin syndrome and/or a hypertensive crisis. Tyramine is broken down by MAO-A, therefore inhibiting its action may result in excessive build-up of it, so diet must be monitored for tyramine intake.

  • MAO-B inhibition reduces the breakdown mainly of dopamine and phenethylamine so there are no dietary restrictions associated with this. Two such drugs, selegiline and rasagiline have been approved by the FDA without dietary restrictions, except in high dosage treatment where they lose their selectivity.

BENEFICIAL USAGE

Chronic use of MAOIs may provide some antidepressant effects that are thought to be mediated by metabolism of tyramine to octopamine, a reaction catalyzed by phenyl-N-methyl transferase that normally converts dopamine to norepinephrine.

**DANGERS OF INTERACTIONS

MAOIs should not be combined with other psychoactive substances (antidepressants, illicit drugs, painkillers, stimulants, etc.) except under expert care. Certain combinations can cause lethal reactions, common examples including SSRIs, tricyclics, MDMA, meperidine, tramadol, and dextromethorphan. Agents with actions on epinephrine, norepinephrine or dopamine must be administered at much lower doses due to potentiation and prolonged effect. Purely opiate-acting analgesics, such as morphine and buprenorphine may be used safely with MAOIs, but may require a dosage adjustment.

IN A NUTSHELL

Basically the particular point that I am trying to bring attention to is the caution that should be taken seriously by those individuals who are on/coming off of a prescribed MAOI. It is better to be safe than sorry AND ALWAYS INFORM your doctor or physician that you are on/ or coming off of an MAOI before recieving prescribed medications or purchasing OTC drugs. As mentioned above, there are certain types of medications that will be metabolized MUCH MUCH SLOWER in the presence of MAOIs, therefore the risk of overdose or toxicity on what would normally be a safe dose of an OTC decongestent could be lethal if takin along with an MAOI regiment. Instead of taking that "normal safe dose" based on weight and age usually, consult your physician just to be safe and SURE THAT you are not putting yourself in harms way.

**SOME MONOAMINE OXIDASE INHIBITORS INCLUDE

(BUT ARE NOT LIMITED TO, ALWAYS ASK A DOCTOR BEFORE MAKING ANY DECISION
)

  • Isocarboxazid (Marplan)
  • Moclobemide (Aurorix, Manerix, Moclodura)
  • Phenelzine (Nardil)
  • Tranylcypromine (Parnate contents 5 mg, Jatrosom contents 10 mg)
  • Selegiline (Selegiline, Eldepryl), and Emsam, Zelapar
  • Rasagiline (Azilect)
  • Nialamide
  • Iproniazid (Marsilid, Iprozid, Ipronid, Rivivol, Propilniazida)
  • Iproclozide
  • Toloxatone
  • Linezolid (Zyvox, Zyvoxid), an antibiotic of the oxazolidinone family, is a reversible, nonselective MAOI which has been known to induce serotonin syndrome post SSRI ingestion. Zyvox requires the same dietary precautions as other MAOI's

  • Many tryptamines have MAOI properties. Harmine (present in Harmal, Banisteriopsis caapi, and tobacco) is a powerful MAOI, which is often used as one of the ingredients of ayahuasca. Certain synthetic tryptamines such as AMT, 5-MeO-DMT or 5-MeO-AMT produce only minor MAO inhibition. The phenethylamine derivatives substituted with a sulfur at the 4-position, such as 2C-T-7 are quite potent MAO-A inhibitors,[5] which makes them potentially dangerous when taken in large doses, or when combined with stimulants such as ephedrine or MDMA "(3,4-methylenedioxy-N-methylamphetamine)", most commonly known today by the street name "Ecstasy". Some deaths have occurred from such combinations.

  • Dienolide kavapyrone desmethoxyyangonin (MAOI-B)[6]
  • Dextroamphetamine [2] "Dexedrine"
  • Methylene blue

</R4NS0M>

Information from Wikipedia

Laughing