Drug breakdown: sertraline

11 November 2021
Drug Breakdown
02 November 2021
Volume 3 · Issue 11

Abstract

In this column, Sharon Rees aims to refresh knowledge and interest in some of the commonly used drugs in a series of tweets. This month she is talking about #sertraline

Dr Sharon Rees @reesprescribe

Day 1: The investigation of tametraline psychoactive compounds led to the discovery of #sertraline in the USA in 1983; not licensed until 1991. Indicated for the treatment and prevention of major depressive episodes, panic disorder, social anxiety disorder, OCD and PTSD. Advantages of #sertraline include being well-tolerated compared to some older SSRIs, with fewer pharmacokinetic drug-drug interactions

Dr Sharon Rees @reesprescribe

Day 2: Oral once-daily dose (if this leads to sleepiness take in the evening) 50-200mg/day depression and OCD; 25-50mg/day panic or social anxiety disorders and PTSD. Children OCD 6-12 years, 25-50 mg/day (can be higher); 13-17 50 mg/day titrate as required. Unlicensed for depression age 12-17, as children are more prone to suicidal thoughts

Dr Sharon Rees @reesprescribe

Day 3: Kinetics #sertraline – Extensive first-pass metabolism includes CYP3A4 and 2C19 breakdown. Half-life 22-36 hours; active metabolite prolongs t½ to 4 days. Renal excretion. Not affected by age or renal impairment, but prolonged t½ in hepatic impairment means caution and avoid if severe. Use of #sertraline in pregnancy carries the risk of birth defects and also withdrawal syndrome in the newborn

Dr Sharon Rees @reesprescribe

Day 4: MOA for #sertraline. This SSRI increases/stabilises brain serotonin levels. The inhibition of the reuptake of serotonin leads to neurotransmitter accumulation and increased signalling across the synapse. This is believed to elevate mood and improve sleep and energy

Dr Sharon Rees @reesprescribe

Day 4 (cont): It can take several weeks for #sertraline to impact depression, but some symptoms can improve sooner, such as anxiety. Some research indicates improving anxiety may be a key mechanism of action for this drug

Dr Sharon Rees @reesprescribe

Day 5: Adverse drug effects: Common include chest pain, GI effects, sweating, dizziness, bleeding risk (inhibits platelet aggregation); Uncommon/rare hallucinations, seizure, diabetes, serotonin syndrome (NOT exhaustive). Caution elderly re hyponatraemia. Many ADEs resolve in few weeks

Dr Sharon Rees @reesprescribe

Day 5 (cont): Increased risk of suicidal ideation is ‘uncertain’ but cannot be ruled out; the highest risk is in the early stages of SSRI treatment in under 25 years. Withdrawal issues can occur as there is adjustment to reduced serotonin levels: SSRI discontinuation syndrome causes chills, insomnia, nightmares, suicidal thoughts. Can lead to rebound symptoms of depression

Dr Sharon Rees @reesprescribe

Day 6: DDIs: All SSRIs, St John's wort, some opioids can lead to serotonin syndrome, cardiovascular medicines re arrhythmias. Increased risk bleeding all anti-platelets/anti-coagulants, NSAIDs. Hyponatraemia with diuretics. Avoid grapefruit juice and other potent CYP3A4 inhibitors increased exposure to #sertraline

Dr Sharon Rees @reesprescribe

Day 7: #sertraline does not cause as much weight gain as some SSRIs, but the reason for this is unclear. SSRI weight gain, in general, may be linked to better appetite and increased energy when mood improved. Also, changes to sodium control/water retention can lead to weight gain

EARN YOUR CPD CERTIFICATE

With the help of Prescribing and Therapeutics Training Ltd and the Journal of Prescribing Practice, you can earn your 1-hour CPD certificate

In addition to the tweets, read the BNF section on antidepressant drugs, as well as the monograph on sertraline. The SPC for sertraline contains useful information about undesirable effects and drug interactions.

Please submit the answers to reesprescribe@gmail.com as a numbered list with TRUE/FALSE or the correct A,B,C,D option. If you achieve 8 or more out of ten on the questions, a CPD certificate will be emailed to you.

Further reading on #sertraline

Questions on sertraline

All SSRIs are derived from tricyclic antidepressants

TRUE or FALSE?

Sertraline is an SSRI associated with less weight gain compared to other SSRI agents

TRUE or FALSE?

Sertraline has the longest half-life of all the SSRIs which means withdrawal issues are unlikely

TRUE or FALSE?

Sertraline is licensed for use for obsessive-compulsive disorder in adults and children

TRUE or FALSE?

What is the mechanism of action for sertraline?

  • It reduces serotonin in the brain
  • It reduces serotonin levels in peripheral nerves
  • It increases serotonin levels in the brain
  • Increases serotonin and dopamine levels in the brain

Sertraline is likely to take effect within the first few days

TRUE or FALSE?

Why is there a caution for use in the elderly?

  • More likely to get addicted
  • Problematic with comorbidities
  • Many drug-drug interactions
  • Can affect electrolyte levels

Grapefruit juice can prevent sertraline from having an anti-depressant effect

TRUE or FALSE?

Which of the following is a rare adverse drug event?

  • Thrombocytopenia
  • Anxiety
  • Dry mouth
  • Yawning

SSRI discontinuation syndrome can cause rebound depression

TRUE or FALSE?