Also known as
Celexa, cipramil, seropram, citadur, nitalapram
Overview
Citalopram is an SSRIselective serotonin reuptake inhibitor. More sold under the brand name Celexa in the United States. Citalopram is indicated for the treatment of a major depressive disorder 1.
Citalopram hydrobromide belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs) 2.
Citalopram is an antidepressive agent that is FDAUS Food and Drug Administration approved for the treatment of depression. There is a Black Box WarningA black box warning is the strictest warning put in the labeling of prescription drugs or drug products by the Food and Drug Administration (FDA) when there is reasonable evidence of an association of a serious hazard with the drug. It is basically a warning with a black box around it, hence the name. Having the black box around the warning means that an adverse reaction to the drug may lead to death or serious injury. More for this drug as shown here. Common adverse reactions include diaphoresisexcessive sweating, constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More, diarrhoeaWhere you frequently pass watery or loose faeces, nausea, vomiting, xerostomiathis is the medical term for a dry mouth due to a lack of saliva. Xerostomia is sometimes colloquially called "pasties" or "cottonmouth". More, dizziness, headache, insomniadifficulty in going to sleep or in getting enough sleep, sedationthe state of being relaxed or sleepy because of a drug More, somnolenceis a state of near-sleep, a strong desire for sleep, or sleeping for unusually long periods. More, tremor, agitation, disorder of ejaculation, fatiguea feeling of weariness, tiredness, or lack of energy. More 3.
Medical usage
Depressive illness, panic disorder 4.
Why take it?
Sought after effects
- relief of anxiety,
- decrease in suicidal thoughts,
- improves general quality of lifethe overall enjoyment of life, a sense of well-being, and the ability to carry out routine activities. More,
- improvements in mood 5.
Undesired effects
- sexual dysfunction,
- loss of appetite,
- hypertensionhigh blood pressure,
- sleep disturbances,
- withdrawal,
- dietary restrictions (for MAOIsMAOIs may be used to treat the symptoms of depression. More) 5.
Dosage
Therapeutic
- By mouth as tablets, depressive illness, 20 mg once daily increased if necessary in steps of 20 mg daily at intervals of 3 – 4 weeks; max. 40 mg daily (elderly over 65 years, max. 20 mg daily).
- Panic disorder, adult over 18 years, initially 10 mg daily increased gradually if necessary in steps of 10 mg daily, usual dose 20 – 30 mg daily; max. 40 mg daily (elderly over 65 years, max. 20 mg daily)
- By mouth as oral drops, depressive illness, 16 mg daily as a single dose increased if necessary in steps of 16 mg daily at intervals of 3 – 4 weeks; max. 32 mg daily (elderly over 65 years, max. 16 mg daily).
- Panic disorder, adult over 18 years, initially 8 mg daily as a single dose increased gradually if necessary in steps of 8 mg, usual dose 16 – 24 mg daily; max. 32 mg daily (elderly over 65 years, max. 16 mg daily) 4.
Abuse
Not known at present.
Abuse
Celexa (citalopram) has been used in combination with moclobemide (an MAOI) to produce euphoriafeelings of joy and happiness 6.
Note – Combining MAOIsMAOIs may be used to treat the symptoms of depression. More with other psychoactive drugs carries serious medical risks and can result in extremely unpleasant side-effects, overheating, nausea, confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation, heart problems, and even death 7.
Pharmacology
Pharmacodynamics
Citalopram is one of a class of antidepressants known as SSRIs. It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of CNSthe Central Nervous System, upon which certain drugs act neuronal uptake of serotonin. in-vitrooutside the body studies show that citalopram is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Citalopram has no significant affinity for adrenergic (α1, α2, β), cholinergic, GABAGamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in your brain, meaning it slows your brain's functions. GABA is known for producing a calming effect., dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptorsnerve endings that sense changes in the body More; antagonism of such receptorsnerve endings that sense changes in the body More has been hypothesised to be associated with various anticholinergic, sedativeOne of a diverse group of drugs manufactured for medical purposes to relax the central nervous system. More, and cardiovascular effects for other psychotropic drugs. The chronic administration of citalopram was found to downregulate brain norepinephrine receptorsnerve endings that sense changes in the body More, as has been observed with other drugs effective in the treatment of major depressive disorder. Citalopram does not inhibit monoamine oxidase 2.
Pharmacokinetics
The single-and multiple-dose pharmacokinetics of citalopram are linear and dose-proportional in a dose range of 10 – 60 mg/day. Biotransformation of citalopram is mainly hepatic, with a mean terminal half-lifethe amount of time required for the amount of something to fall to half its initial value of about 35 hours. With once daily dosing, steady state plasma concentrations are achieved within approximately one week. At steady state, the extent of accumulation of citalopram in plasma, based on the half-lifethe amount of time required for the amount of something to fall to half its initial value, is expected to be 2.5 times the plasma concentrations observed after a single dose 8.
Absorption
Rapidly and well absorbed from the gastrointestinal tract. Peak plasma concentrations occur within 4 hours of a single orally administered dose. Food does not affect absorption 2.
Bioavailability
Bioavailability is 80% following oral administration 2.
Metabolism
Citalopram is metabolised mainly in the liver via N-demethylation to its principle metabolite, demethylcitalopram. Other metabolites include didemethylcitalopram, citalopram N-oxide, and a deaminated propionic acid derivative. However, the predominant entity in plasma is unchanged citalopram. Cytochrome P450 (CYP) 3A4 and 2C19 isozymes appear to be principally involved in producing demethylcitalopram. Demethylcitalopram appears to be further N-demethylated by CYP2D6 to didemethylcitalopram. Citalopram metabolites possess little pharmacologic activity in comparison to their parent compound and do not likely contribute to the clinical effect of the drug 2.
Half-life
35 hours 2.
Elimination
12% – 23% of an oral dose of citalopram is recovered unchanged in the urine, while 10% of the dose is recovered in the faeces 2.
Lethal dosage
Toxicity
Symptoms most often accompanying citalopram overdose, alone or in combination with other drugs and/or alcohol, included dizziness, sweating, nausea, vomiting, tremor, somnolenceis a state of near-sleep, a strong desire for sleep, or sleeping for unusually long periods. More, and sinus tachycardiarapid pulse rate. In more rare cases, observed symptoms included amnesiainability to remember, confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation, coma, convulsionswhen your body shakes violently without you meaning it to, hyperventilation, cyanosisbluish tinge to fingers and lips, caused by inadequate blood supply, rhabdomyolysisa condition that may occur when muscle tissue is damaged due to an injury in which muscle in the body is damaged More, and ECGelectrocardiogram, a machine that makes a record of the electrical conductivity of the heart. More changes (including QTc prolongation, nodal rhythm, ventricular arrhythmiavariation or irregularity of the rhythm of the heart More, and very rare cases of torsade de pointes). Acute renal failure has been very rarely reported accompanying overdose. Withdrawal symptoms include flu-like symptoms, insomniadifficulty in going to sleep or in getting enough sleep, nausea, imbalance, sensory changes and hyperactivity 2.
Mechanism of action
The antidepressant, antiobsessive-compulsive, and antibulimic actions of citalopram are presumed to be linked to its inhibition of CNSthe Central Nervous System, upon which certain drugs act neuronal uptake of serotonin. Citalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptorsnerve endings that sense changes in the body More than tricyclic antidepressant drugs 2.
Carcinogenesis, mutagenesis, impairment of fertility
There was no evidence of carcinogenesis in mice given 20 times the recommended human dose. There was an increased risk of small intestine carcinomaa cancer that begins in a tissue that lines the inner or outer surfaces of the body. More in rats given 1.3 to 4 times the recommended human dose. Certain in-vitrooutside the body studies found evidence of mutagenicityhaving the capacity to induce mutations. More while others did not.
Rats fed citalopram experienced decreased mating and fertility. It is not known what implication these animal studies have for humans 9.
Signs of usage
- Stealing, forging or selling prescriptions,
- Taking higher doses than prescribed,
- Excessive mood swings or hostility,
- Increased or decreased need of sleep,
- Confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation and poor decision-making,
- Appearing to be high, unusually energetic or revved up, or sedated,
- Continually “losing” prescriptions, so more prescriptions must be written,
- Seeking prescriptions from more than one doctor or “doctor shopping” 10.
Effects
More common
- drowsiness,
- dryness of mouth,
- nausea,
- trouble in sleeping 11.
Less common
- abdominal pain,
- anxiety,
- change in sense of taste,
- diarrhoeaWhere you frequently pass watery or loose faeces,
- wind,
- headache,
- heartburn,
- increased sweating,
- increased yawning,
- loss of appetite,
- pain in muscles or jointsmarijuana cigarettes More,
- stuffy or runny nose,
- tingling, burning, or prickly feelings on skin,
- tooth grinding,
- trembling or shaking,
- unusual increase or decrease in weight,
- unusual tiredness or weakness,
- vomiting,
- excessive salivation 11.
Minor side-effects
Some of the side-effects that can occur with citalopram may not need medical attention. As your body adjusts to the medicine during treatment these side-effects may go away. Your health care professional may also be able to tell you about ways to reduce or prevent some of these side-effects 12. If any of the following side-effects continue, are bothersome or if you have any questions about them, check with your health care professional –
More common
- decrease in sexual desire or ability,
- sleepiness or unusual drowsiness 12.
Less common
- body aches or pain,
- change in sense of taste,
- wind,
- headache (severe and throbbing),
- heartburn,
- increased sweating,
- increased yawning,
- loss of voice,
- pain in the muscles or jointsmarijuana cigarettes More,
- sneezing,
- stuffy or runny nose,
- tingling, burning, or prickly feelings on the skin,
- tooth grinding,
- unusual increase or decrease in weight,
- watering of the mouth 12.
Incidence not known
- bruising,
- inability to sit still,
- large, flat, blue or purplish patches in the skin,
- need to keep moving,
- uncontrolled eye movements 12.
Major side-effects
You should check with your doctor immediately if any of these side-effects occur when taking citalopram –
Less common
- agitation,
- blurred vision,
- confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation,
- fever,
- increase in the frequency of urination or amount of urine produced,
- lack of emotion,
- loss of memory,
- menstrual changes,
- skin rash or itching,
- trouble breathing 12.
Rare
- behaviour change similar to drunkenness,
- bleeding gums,
- breast tenderness or enlargement or unusual secretion of milk (in females),
- chills,
- convulsionswhen your body shakes violently without you meaning it to (seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More),
- diarrhoeaWhere you frequently pass watery or loose faeces,
- difficulty with concentrating,
- dizziness or fainting,
- drowsiness,
- increased hunger,
- increased thirst,
- irregular heartbeat,
- lack of energy,
- lethargy,
- nosebleed,
- overactive reflexes,
- painful urination,
- poor coordination,
- purple or red spots on the skin,
- rapid weight gain,
- red or irritated eyes,
- redness, tenderness, itching, burning, or peeling of the skin,
- shivering,
- slow or irregular heartbeat (less than 50 beats per minute),
- sore throat,
- stupor,
- sweating,
- swelling of the face, ankles, or hands,
- talking or acting with excitement you cannot control,
- trembling, shaking, or twitching,
- trouble with holding or releasing urine,
- unusual or sudden body or facial movements or postures,
- unusual tiredness or weakness 12.
Incidence not known
- abdominal or stomach pain,
- back or leg pains,
- black, tarry stools,
- bloating,
- bloody stools,
- chest pain,
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More,
- cough,
- darkened urine,
- difficult or fast breathing,
- difficulty with swallowing,
- drooling,
- fast, slow, or irregular heartbeat,
- general body swelling,
- hive-like swelling on the face, eyelids, lips, tongue, or throat,
- hivesThis is an allergic skin reaction causing localised redness, swelling, and itching.,
- holding false beliefs that cannot be changed by fact,
- impaired consciousness, ranging from confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation to coma,
- indigestion,
- itching, puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue,
- jaundiceyellowing of your skin or the whites of your eyes,
- loss of appetite,
- loss of bladder control,
- loss of consciousness,
- medical confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation (which is confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation as to time, place, or person),
- muscle cramps or spasms,
- muscle tightness,
- muscle twitching or jerking,
- pale skin,
- penile erections, frequent or continuing,
- recurrent fainting,
- rhythmic movement of the muscles,
- seeing, hearing, or feeling things that are not there,
- swelling of the breasts or unusual milk production,
- tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over the affected area,
- tightness in the chest,
- total body jerking,
- twitching, twisting, uncontrolled repetitive movements of the tongue, lips, face, arms, or legs,
- uncontrolled jerking or twisting movements,
- unusual excitement,
- vomiting of blood or material that looks like coffee grounds 12.
Overdose
- dizziness,
- drowsiness,
- fast heartbeat,
- nausea,
- sweating,
- trembling or shaking,
- vomiting,
- cyanosisbluish tinge to fingers and lips, caused by inadequate blood supply,
- confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation,
- convulsionswhen your body shakes violently without you meaning it to (seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More),
- coma,
- deep or fast breathing with dizziness,
- fainting,
- general feeling of discomfort or illness,
- loss of memory,
- muscle pain,
- slow or irregular heartbeat,
- weakness 11.
Risks
Black Box Warning
The FDAUS Food and Drug Administration released a black box warningA black box warning is the strictest warning put in the labeling of prescription drugs or drug products by the Food and Drug Administration (FDA) when there is reasonable evidence of an association of a serious hazard with the drug. It is basically a warning with a black box around it, hence the name. Having the black box around the warning means that an adverse reaction to the drug may lead to death or serious injury. More in 2007, cautioning that the usage of SSRIs may lead to increased suicidal thoughts and behaviours. The FDAUS Food and Drug Administration warned that this problem can be especially problematic for adolescents and young adults who are on SSRIs. Doctors who prescribe SSRIs, including Celexa, must be cautious and observe patients for declining mood or thoughts of suicide, especially for young people just beginning their prescription 11.
Withdrawal
After abusing Citalopram for a period of time, a Citalopram psychological dependency could develop. Citalopram, like other antidepressants, is not considered to be addictive. However, if a person continues abusing Citalopram and suddenly discontinues taking the drug, something called SSRIselective serotonin reuptake inhibitor. More discontinuation syndrome may be experience. SSRIselective serotonin reuptake inhibitor. More discontinuation syndrome produces harsh withdrawal symptoms that happen when a person suddenly stops taking the drug, decreases the dose too rapidly, or even after skipping an individual dose 13. These are –
- vivid dreaming,
- nausea,
- depression,
- suicidal thoughts,
- panic attack,
- sexual dysfunction,
- cardiac arrhythmiavariation or irregularity of the rhythm of the heart More,
- frequent urination,
- memory problems,
- tremors,
- confused thinking 13.
Some of the consequences that may be experienced 13.
- anxiety,
- dizziness,
- nervousness,
- trembling or shaking 11.
History
Citalopram was approved in 1998 by the FDAUS Food and Drug Administration for the treatment of major depressive disorder 14. Citalopram is almost exclusively found as the hydrobromide salt, which is the only form approved by the FDAUS Food and Drug Administration 12.
Celexa (citalopram hydrobromide) was introduced in 1998 to treat depression 15.
Footnotes:
Selective serotonin reuptake inhibitor, 2017, https://psychonautwiki.org/wiki/Selective_serotonin_reuptake_inhibitor
Citalopram, 2017, https://www.drugbank.ca/drugs/DB00215
Citalopram, 2015, http://www.wikidoc.org/index.php/Citalopram
Antidepressants, 2017, https://wiki.tripsit.me/wiki/Antidepressants
Neuvonen, P. J. and Pohjola-Sintonen, S. and Tacke, U. and Vuori, E., Five fatal cases of serotonin syndrome after moclobemide-citalopram or moclobemide-clomipramine overdoses (letter), Lancet, 1993, 342, 8884, 1419, https://www.ncbi.nlm.nih.gov/pubmed/7901695
Sewell, R. A., Recreational Use of SSRIs and Other Antidepressants, 2007, https://www.erowid.org/chemicals/ssris/ssris_info2.shtml
Celexa, 2017, http://www.rxlist.com/celexa-drug.htm
Schimelpfening, N., Citalopram (Celexa) Antidepressant, 2016, https://www.verywell.com/citalopram-celexa-1065169
Prescription Drugs, 2017, http://www.saveoursociety.org/the-issues/prescription-drugs/
Purse, M., Celexa (Citalopram) Medication Profile, 2017, https://www.verywell.com/celexa-citalopram-medication-profile-379761
Citalopram, 2017, https://www.drugs.com/citalopram.html
Ekern, J., Celexa Abuse Causes, Statistics, Addiction Signs, Symptoms & Side Effects, 2015, https://www.addictionhope.com/celexa/
Nemeroff, C. B., Management of Treatment-Resistant Major Psychiatric Disorders, 2012, Oxford University Press, P 30.
Mauney, M., Celexa, 2017, https://www.drugwatch.com/celexa/