It’s natural for people to prefer being healthy over being sick, which prompts them to be responsible with their medication. In some cases, people might take an extra pill to achieve wellness sooner, but that extra pill might be harmful more than helpful. Why? The human body can only tolerate a certain amount of drugs, so the accumulation of medicine could start to harm and disturb your body’s systems. It’s similar to cooking, you can put salt into your food as much as you want, but at a certain point you overshoot the ideal amount of salt, and the food becomes too salty to be enjoyable.

Before we can understand the role of the pKa in drug overdosing, we need to understand the concept of pKa and its effects on absorption and excretion. pKa is a value that indicates the acidity and basicity in a balanced aqueous solution. To absorb the medicine you take, the molecules inside the drug must not have an electrical charge, which allows them to pass through our membrane.

 

4

 

Specifically, the electrical charge of the medicine is dependent upon the pKa of itself and the surrounding pH [1].For example, acidic medicines are uncharged around acidic compartments and basic medicines are uncharged around basic compartments, allowing them to cross the membrane. On the other hand, acidic drugs will become charged when surrounded by basic compartments and cannot be absorbed anymore. This is similar to basic drugs, which will become charged when surrounded by acidic compartments.

By knowing the pKa of a drug and pH of certain body compartment, you will able to calculate how many drugs will be electrically charged or not, excreted or absorbed by using Henderson–Hasselbalch equation:
2

 

How do drugs leave our body system? Drug are usually filtered out by the renal tubule, which is in the kidney. Electrically charged molecules inside can easily slip out, but uncharged molecules are reabsorbed back into the bloodstream and continue affecting your body [4].

3

 

If you overdose on a drug, these extra uncharged molecules will start to disturb your body’s systems [3]. To minimize the damage, the doctor might administer medicine that affects the pH of your blood. In the case of overdose methamphetamine, ammonium chloride can be used to lower the pH of the patient’s urine which electrically charges the methamphetamine molecules [3]. Eventually, these charged molecules will remain in the renal tubule and pass out of the body through urination.

 

3
Figure: Mean cumulative urinary excretion of methamphetamine (11 mg oral dose) in men as a function of urine pH. [Beckett AH. Rowland M 1965]

 

In conclusion, medicine can both improve and worsen a person’s wellbeing. Hopefully, this explanation of pKa will give you a general idea of how medicine works and a heightened sense of caution when managing your medicine.

 

 

 

 

 

 

 

 

 

 

 

 

 

Reference List

[1] Count Dracula 2015, Science, ‘Role of ph and pka in Drug Absorption‘ viewed on 26 April 2018, < https://drugs-bd.blogspot.com.au/2015/04/role-of-ph-and-pka-in-drug-absorption.html?q=pKa>

[2] David, T. M. 2007, ‘The pKa distribution of drugs: application to drugs discovery’, National Center for Biotechnology Information, vol. 1, pp 25-38.

[3] Pharmwiki 2010, ‘pH effect on drug elimination’, viewed on 26 April 2018,<http://tmedweb.tulane.edu/pharmwiki/doku.php/ph_effect_on_drug_elimination>

[4] Raymond, J.S.H.& Neill, J. 1997. Influence of pH on drug absorption from the gastrointestinal tract: a simple chemical model’, Journal of Chemical Education, vol. 75, n. 7, pp855.

Image:

[5] Beckett, A.H. & Rowland, M. 1965, Mean Cumulative Urinary Excretion of Methamphetamine (11 mg oral dose) in Men as a Function of Urine pH,  Pharmwiki, <http://tmedweb.tulane.edu/pharmwiki/doku.php/ph_effect_on_drug_elimination>

 

 

 

 

 

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