Category: MD2140 (page 2 of 6)

Why are peripheral effects of AChE inhibitors predominantly parasympathomimetic?

Acetylcholinesterase (AChE) inhibitors will prevent the breakdown of acetylcholine (ACh) and so increase ACh levels. Increased ACh levels at autonomic nervous system ganglia should activate both the sympathetic and parasympathetic nervous systems. However, the adverse effects of AChE inhibitors outside of the CNS are mostly parasympathomimetic. Why do AChE inhibitors not stimulate the sympathetic nervous system as well?

Acetylcholinesterase (AChE) inhibitors increase the concentration of acetylcholine (ACh) at synapses by blocking its breakdown. This will activate both the sympathetic and parasympathetic systems, as the preganglionic neurons in both systems release ACh.

However, the impact of AChE inhibitors is more prominent on the parasympathetic nervous system for several reasons:
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When sympathetic and parasympathetic systems collide: The dominance of excitatory effects

When the autonomic nervous system ganglia are activated (for example, by low-dose nicotine), both the sympathetic and parasympathetic nervous system innervations of target organs and tissues are simultaneously stimulated. However, the “fright, fight or flight” sympathetic and “rest and digest” parasympathetic nervous systems have opposing effects in most target organs and tissues. So why do the sympathetic and parasympathetic nervous systems not just cancel each other out when activated at the same time?

It is true that in the realm of autonomic nervous system functioning, the sympathetic and parasympathetic systems often represent two sides of the same coin. These systems largely produce opposing effects on the same target organs and tissues. However, what happens when both systems are simultaneously activated? Contrary to intuitive thinking, they don’t simply cancel each other out. Instead, the dominion of activation or excitatory effects takes centre stage.

The Principle of Dominant Excitation: When both the sympathetic and parasympathetic systems are co-activated, it isn’t a zero-sum game. Rather than neutralizing each other, the excitatory effects from each system generally prevail. This principle is observed in a variety of physiological contexts. Continue reading

Why is hydroxychloroquine used for systemic lupus erythematosus (SLE)?

Why is an antimalarial drug, hydroxychloroquine, used as a rheumatological immunosuppressant in disorders such as systemic lupus erythematosus (SLE)?

Hydroxychloroquine (HCQ), originally developed as an antimalarial, has become a cornerstone in the treatment of autoimmune diseases, including systemic lupus erythematosus (SLE), primary Sjögren’s syndrome, and rheumatoid arthritis. How does this drug help address the challenges posed by these autoimmune diseases?

1. Interference with lysosomal activity and autophagy:
HCQ increases the pH within intracellular lysosomes, interrupting the autophagy of macromolecules and antigen processing in antigen-presenting cells. This leads to diminished T cell stimulation, providing an advantage in autoimmune conditions like SLE by modulating immune responses.

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Why do corticosteroids increase circulating neutrophils?

Corticosteroids are anti-inflammatory, reducing the number and activity of various inflammatory cell types, including lowering blood lymphocyte, monocyte, and basophil counts and preventing neutrophils from reaching sites of inflammation. So why do corticosteroids increase the number of neutrophils in circulation? 

The effects of corticosteroids reducing the infiltration of neutrophils to sites of inflammation within tissues and increasing the number of neutrophils staying in circulation are two sides of the same mechanism.

Surface expression of proteins, such as L-selectin, is involved in the rolling capture and adherence of neutrophils to blood vessel walls, which is necessary to enable extravasation through blood vessel walls and migration into tissues. Corticosteroids acting via glucocorticoid receptors regulate the expression of many genes involved in inflammatory responses. Continue reading

Thiazide diuretics and hypercalcaemia

Why is it said that thiazide diuretics may unmask hypercalcemia?

Thiazide diuretics increase the risk of hypercalcaemia. There are several mechanisms by which they have been reported to contribute to increased serum calcium levels, but most important is that they increase renal tubular reabsorption of calcium resulting in reduced calcium excretion in urine. Normally, this is not a problem for otherwise healthy individuals. However, thiazide diuretics are contraindicated in patients at risk of hypercalcaemia, for example, because of primary hyperparathyroidism or sarcoidosis.

Primary hyperparathyroidism is the most common cause of hypercalcaemia. Excessive secretion of parathyroid hormone (PTH), a key factor in calcium metabolism, results in the leaching of calcium from bone and increased production of calcitriol, the active form of Vitamin D, which increases intestinal absorption of calcium and reabsorption in the kidneys. Sarcoidosis is clinically observed to be associated with increased risk of hypercalcaemia, which is most frequently explained by overproduction of calcitriol by activated macrophages.

PPIs and C. difficile infection

Does the use of proton-pump inhibitors (PPIs) increase the risk of Clostridioides difficile infection?

Medical literature has debated whether PPIs increase the risk of C. difficile enteric infections for many years. Analysis of the issue has been complicated because proton-pump inhibitors are often taken together with antibiotics in triple therapy to eradicate Helicobacter pylori. Antibiotics can alter the normal gut microbiota allowing the proliferation of C. difficile. 

While the pathophysiological mechanisms remain unknown, the evidence increasingly supports the conclusion that PPIs increase the risk of C. difficile infection even without antibiotic use (Wolfe et al., 2021). There is a greater risk of C. difficile infection with PPIs than H2 receptor blockers (Kwok et al., 2012; Leonard et al., 2007). Although there is considerable variation among studies, overall PPIs also increase the risk of recurrent C. difficile infection (Kwok et al., 2012; Tariq et al., 2017).
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Folate, folic acid or folinic acid to reduce adverse effects of methotrexate?

What is the difference between folate, folic acid, and folinic acid? And how do each of them contribute or are involved in the methotrexate pathway?

Folate is the naturally occurring salt form of vitamin B9. Folic acid is a synthetic water-soluble acid form of vitamin B9. Folate and folic acid are metabolised by dihydrofolate reductase, the enzyme inhibited by methotrexate, to FH2 and then FH4, which in turn is converted to N5, N10-methylene-FH4.

Folinic acid (also known as leucovorin) is N5-formyl-FH4 and can be converted rapidly to N5, N10-methylene-FH4 without the need for dihydrofolate reductase and so bypasses the inhibition of the pathway by methotrexate.

In the treatment of rheumatoid arthritis with methotrexate, adverse effects include nausea and vomiting, mouth and gastrointestinal ulcers, and hair loss are caused by the reduction in N5, N10-methylene-FH4, which is required for the synthesis of amino acids and nucleic acids necessary for cell proliferation.  Folic acid at high enough doses to overcome the methotrexate inhibition of dihydrofolate reductase or folinic acid is therefore used to reduce the adverse effects of methotrexate.

Dose-dependence of COX-2 selectivity of coxibs

Coxibs are pro-thrombotic, but if given at a high dose, there would be COX-1 inhibition resulting in an antiplatelet effect and hence bleeding would occur. Therefore, would the two effects not cancel each other out, or would the prothrombic effect still be the predominant effect?

The pro-thrombotic effect still dominates since, for coxibs, the COX-2 inhibition is always more than the COX-1 inhibition.

Coxibs are selective inhibitors of COX-2. Selective inhibition of COX-2 results in shunting of the precursor arachidonic acid over to the COX-1 pathway. With COX-2 inhibited and COX-1 functional, there is a relative increase in the ratio of the thromboxane A2 (TXA2) produced via COX-1 to prostaglandin I2 (PGI2) or prostacyclin produced via COX-2, and also in some cell types via COX-1. As TXA2 promotes platelet aggregation, while PGI2 inhibits platelet aggregation, the increased ratio of TXA2 over PGI2 favours platelet aggregation, so there is an increased risk of thrombosis.

Although coxibs are selective for COX-2, the selectivity is dose-dependent. Therefore, at higher doses, there will be more inhibition of COX-1. However, in the case of the balance between the risk of thrombosis versus the risk of bleeding, there is little impact because, as the dose increases, there will still be more inhibition of COX-2 than COX-1. So the ratio of TXA2 to PGI2 remains in favour of thrombosis.

Importantly, the dose-dependence of the selectivity for COX-2 is significant with regards to the gastrointestinal adverse effects. A major advantage of the coxibs is that they have a lower risk of upper gastrointestinal tract (GIT) adverse effects as they do not inhibit COX-1 in the stomach. However, if the dose is increased, there is greater inhibition of COX-1 and, therefore, less sparing from upper GIT adverse effects.

Choice of NSAID for closure of patent ductus arteriosus?

Why is indometacin a drug of choice for closing the ductus arteriosus post-partum? As the ductus arteriosus is kept open by PGE2, may I know why other NSAIDs or paracetamol are not as ideal for this purpose?

The ductus arteriosus allows blood to bypass the lungs in utero but should close after birth. Cyclo-oxygenase-2 (COX-2) mediated production of prostaglandin E2 (PGE2) is important in keeping the ductus arteriosus open in utero. Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit COX-2 when administered at analgesic and anti-inflammatory doses. Therefore, the risk of premature closure of the ductus arteriosus is one reason for the contraindication of NSAIDs in the third trimester of pregnancy.

Patent ductus arteriosus (PDA) occurs when the ductus arteriosus fails to close after birth. NSAIDs can help to close the PDA. Older NSAIDs are typically used because there is a longer history of use and so better knowledge of the risks in infants. Either indometacin, also known as indomethacin (USAN), or ibuprofen is usually used. Paracetamol has also been used as it is has been considered safer in young children. It is not as effectively or widely used, but that it works at all shows that paracetamol can in certain situations inhibit COX-2 in vivo outside of the CNS. Newer NSAIDs are typically not preferred as clinical trials rarely include newborn infants, and so their safety in infants is poorly understood.

Route of administration of N-acetylcysteine for paracetamol poisoning

In a clinical setting of paracetamol poisoning, how would N-acetylcysteine be administered to the patient? 

It is usually administered intravenously (IV). It is best administered within 8 hrs of paracetamol overdose, and dosing is maintained over the next 20 hrs.

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