Does Citalopram cross the blood-brain barrier? (+3 factors)
By
Ivan Kahwa
Author bio
Mr Ivan Kahwa is a chemist and phytopharmaceutical scientist with expertise in chemistry, pharmacology, phytochemistry, and Nanobiotechnology. He writes and reviews content on these topics.
Mr Ivan Kahwa’s Highlights:
Guest Researcher at the University of Leipzig, Senior Research Fellow/Scientist, and Lecturer at the Department of Pharmacy, Faculty of Medicine, Mbarara University of Science and Technology.
Professional Experience:
Mr Ivan joined PHARMBIOTRAC as a research fellow/scientist during his master of science tenure. He contributed to the development of most of the phytopharmaceutical products in the project. Furthermore, he participated in carrying out the pharmacological activities of the developed products in laboratory animals such as mice and rats in order to develop proper doses hence leading to pre-clinical studies.
With the above relevant research experience, Ivan started to work with the University of Leipzig on collaborative projects with Mbarara University to develop the chemistry of Ugandan Medicinal plants and their pharmacological activities. This was coupled with several consultative positions by different German NGOs. Mr. Kahwa is also a supporting in the teaching and learning at the Departments of Pharmacy and Pharmaceutical Sciences, Faculty of Medicine, Mbarara University of Science and Technology.
With the increase in antimicrobial resistance globally, Ivan retooled his thinking towards developing new naturally derived antibiotic regimens from Ugandan propolis with the assistance of nanotechnology to improve their delivery to microbial cells. Kahwa has also published over 28 articles in peer-reviewed journals and he is currently reviewing for many journals.
Education:
2023-2027: PhD in Pharmaceutical Sciences (ongoing) with a focus on Pharmaceutical Microbiology and Nanobiology at Mbarara University of Science and Technology.
2022: 2Msc. in Pharmacognosy and Natural Medicine Science at Mbarara University of Science and Technology.
2018: Bachelor of Science (Chemistry) at Mbarara University of Science and Technology.
Publications:
▪ Iqbal, S., Jabeen, F., Kahwa, I., & Omara, T. 2023. Suberosin Alleviates Thiazolidinedione-Induced Cardiomyopathy in Diabetic Rats by Inhibiting Ferroptosis via Modulation of ACSL4-LPCAT3 and PI3K-AKT Signaling Pathways. Cardiovascular Toxicology. https://doi.org/10.1007/s12012-023-09804-7
▪ Gupta, A. K., Yadav, R., Sharma, S., Sawale, J., & Kahwa, I. 2023. Anti-ageing Activity and Antioxidant Activity of Methanol Extracts of Leaves and Flowers of Salvia officinalis and Rosmarinus officinalis. Journal of Young Pharmacists, 15(3), 448–455. https://doi.org/10.5530/jyp.2023.15.60
▪ Tolo, C.U., Kahwa, I., Nuwagira, U., Weisheit, A. and Ikiriza, H., 2023. Medicinal plants used in treatment of various diseases in the Rwenzori Region, Western Uganda. Ethnobotany Research and Applications, 25, pp.1-16.
https://ethnobotanyjournal.org/index.php/era/article/view/4683
▪ Kahwa, I., Ajayi, C.O., Yadav, R., Chauhan, N.S., Shah, K., Abdelgadir, A.A., Shegena, E.A., Daniel, S., Omara, T., Asiimwe, J.B. and Ikiriza, H., 2023. Pharmacognostic and phytochemical studies as an invaluable approach for correct identification of medicinal plants: The case of Artemisia vulgaris L. substituted for Artemisia annua L. in Western Uganda. TMR Integr Med, 7, p.e23004.
https://doi.org/10.53388/TMRIM202307004
▪ Nalimu, F., Oloro, J., Kahwa, I. and Ogwang, P.E., 2021. Review on the phytochemistry and toxicological profiles of Aloe vera and Aloe ferox. Future Journal of Pharmaceutical Sciences, 7, pp.1-21.
https://doi.org/10.1186/s43094-021-00296-2
▪ Elamin, O.H.S., Ali, M.A., Elgezuli, I.A.A., Bashir, M.A. and Kahwa, I., 2021. Diagnosis of pre-and post-treatment of echinococcus granulosus with counter current immune electrophoresis and bacterial co-agglutination. Journal of Microbiology and Infectious Diseases, 11(02), pp.88-94.
https://doi.org/10.5799/jmid.951600
Published book Chapter
▪ Kahwa, I., Ayesiga, I., Nakalema, S., Alinaiswe, R., Mbabazi, R. and Iqbal, S., 2023. Natural products in the management of onchocerciasis. In Natural Products in Vector-Borne Disease Management (pp. 63-80). Academic Press. Book Chapter.
https://doi.org/10.1016/B978-0-323-91942-5.00012-4
Submitted manuscripts Under Review:
▪ Comparison of the Wound Healing Activity of the Leaf and Leaf Ash Extracts of Vernonia amygdalina in Rats. Journal name: Clinical Phytoscience
▪ Ethnobotanical Survey of Medicinal plants used in the management of cancer in Uganda. Journal name: Journal of Herbal Medicine
▪ Ethnobotanical survey and phytochemical screening of medicinal plants used in treatment of epilepsy by PROMETRA-Uganda Traditional Health Practitioners in Mpigi District, Uganda. Journal name: Journal of Ethnopharmacology
Submitted book chapters under review
1.Book title: Algae as a Natural Solution for Water-Food-Energy Nexus, Section 4: Microalgae and cyanobacteria for food applications, Chapter 4.6: Safety, toxicological and allergenic aspects of using algae for food. Authors: Christine Kyarimpa, Tom Omute, Caroline K. Nakiguli, Alice V. Khanakwa4, Christopher Angiro, Ivan Kahwa, Fortunate Ahumuza, Timothy Omara*. Publisher: Springer Nature Singapore Pte Ltd. 152 Beach Road, #21-01/04 Gateway East, Singapore 189721, Singapore.
2.Book title: Nutraceuticals Inspiring the Contemporary Therapy for Lifestyle Diseases. Chapter: Nutraceutical applications of Seaweeds and their Phytocompounds in Nutrition and Treatment of Diseases. Authors: Ivan Kahwa, Timothy Omara , Innocent Ayesiga , Gael Noel Neh Neba Ambe , Zehbanaz Javidbhai Panwala , Rachel Mbabazi , Shabnoor Iqbal , Christine Kyarimpa , Christine Betty Nagawa , Kamal Shah ,Nagendra Singh Chauhan* Publisher: CRC Press
You can view my works on the following professional sites:
Research Gate: https://www.researchgate.net/profile/Ivan-Kahwa
Google Scholar: https://scholar.google.com/citations?user=tOwrvqoAAAAJ&hl=en
ORCID: https://orcid.org/0000-0002-6440-3437
Linkedin: https://de.linkedin.com/in/ivan-kahwa-865450159
In this article, we will answer whether Citalopram crosses the blood-brain barrier or not. We will further look into the common pathway of Citalopram as an SSRI antidepressant. We will also provide an overview of the factors affecting the penetration across the BBB.
Does Citalopram cross the blood-brain barrier?
Yes, Citalopram can cross the blood-brain barrier (BBB). Citalopram is an SSRI antidepressant and works by inhibiting the reuptake of serotonin in the brain, therefore, it can cross the BBB.
Citalopram, like other antidepressants, enters the brain and increases serotonin levels which helps in regulating mood and treating anxiety, depression, and other related conditions.
How does Citalopram penetrate the BBB?
Citalopram penetrates the blood-brain barrier (BBB) due to its chemical structure and mechanism of action among other SSRI antidepressants. It is a highly potent and selective SSRI drug (1).
Based on the chemical structure of this drug, Citalopram is a racemic drug and its therapeutic activity lies in the S-enantiomer whereas, the R-enantiomer is practically devoid of serotonin reuptake (1,2).
Depending upon the chemical structure, Citalopram does not directly affect the integrity of the BBB. But once it enters the brain, it acts on serotonin transporters, improves mood regulation, and treats anxiety and depression-related conditions.
Neuropsychiatric drugs consist of drug-bound and unbound concentrations. Similar to other psychoactive drugs, Citalopram is also bound to plasma proteins. It is assumed that only the unbound fraction of Citalopram can passively cross the BBB (1).
The protein binding varies based on individual factors like metabolism, liver function, polypharmacy, etc. Therefore, Citalopram should be prescribed to patients after considering such factors.
However, it is suggested that Citalopram crosses the BBB via a non-stereoselective, bidirectional, and symmetrical carrier-mediated mechanism. This occurs without the influence of active efflux mechanisms (3).
Factors that affect the permeability of Citalopram across the BBB
Following are a few factors that affect the permeability of Citalopram across the BBB (1,3):
Molecular size and Active transport
The molecular size and structure of Citalopram greatly affect its ability to cross the BBB. Preferably, the smaller molecules of Citalopram are more likely to cross the BBB readily.
The serotonin transporters in the brain significantly play an important role in helping the Citalopram molecules to cross the BBB.
The high concentrations of Citalopram in the cerebrospinal fluid indicate an active transport of Citalopram into the brain. This results in higher drug concentration at target sites which contribute towards the clinical efficacy (1).
Protein binding and Lipophilicity
Protein binding is another important factor in the penetration of Citalopram across the BBB. Highly bound drugs have fewer unbound molecules to freely cross the BBB and exert their effects on the brain.
The lipophilicity or the ability of the drug molecules to dissolve in lipids is a plus point for Citalopram to cross the BBB. The lipophilic drugs tend to cross the BBB more readily as compared to the hydrophilic drugs.
How to ensure the safe use of Citalopram?
You can ensure safe and effective use of Citalopram by following the exact dosage strength and frequency of the drug prescribed by your health care provider. Do not change or miss the dosage recommended by the doctor.
Monitor your side effects regularly. It is essential to familiarize yourself with the potential side effects of Citalopram. If you face severe adverse effects, do not abruptly stop taking the medication or go cold turkey. Instead, consult your doctor for a dosage reduction or a medication switch.
Never miss your follow-up sessions with your doctor. Also, educate yourself about the potential drug interactions, adverse effects, and risks of taking psychotropic drugs such as Citalopram.
Avoid alcohol consumption along with Citalopram. It enhances the sedative side effects and also increases the potential risk factors. Therefore, it is advised to avoid alcohol and other intoxicants while being on Citalopram.
Conclusion
We have answered that Citalopram can cross the blood-brain barrier. We have successfully discussed the role of Citalopram in the brain and its capacity to penetrate the BBB to perform its function. We have also discussed the factors that affect the penetration of Citalopram across the BBB.
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References
1.-
Paulzen, M., Lammertz, S. E., Gründer, G., Veselinovic, T., Hiemke, C., & Tauber, S. C. (2016). Measuring citalopram in blood and central nervous system. International Clinical Psychopharmacology, 31(3), 119–126. doi: 10.1097/yic.0000000000000114 https://pubmed.ncbi.nlm.nih.gov/26650488/
2.-
Sangkuhl K, Klein TE, Altman RB. PharmGKB summary: citalopram pharmacokinetics pathway. Pharmacogenet Genomics. 2011 Nov;21(11):769-72. doi: 10.1097/FPC.0b013e328346063f. PMID: 21546862; PMCID: PMC3349993. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3349993/
3.-
Rochat B, Baumann P, Audus KL. Transport mechanisms for the antidepressant citalopram in brain microvessel endothelium. Brain Res. 1999 Jun 12;831(1-2):229-36. doi: 10.1016/s0006-8993(99)01461-4. PMID: 10412001. https://pubmed.ncbi.nlm.nih.gov/10412001/
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