The medication chapters in this book provided general information about several classes of psychotropic medications.
With that knowledge in mind, this appendix provides an introduction to specific medications within these general classes. For each medication, we list basic information and share what we consider are the things that differentiate it from other medications in the same class. This will help you begin to compare your options. Some of the resources mentioned in Appendix A will give much greater detail.
Here are a few things to keep in mind in order to make the best use of this material.
Medication selection. We only include a subset of the several dozen psychotropic medications in use today. We’ve chosen those that are either commonly used or are particularly effective for specific problems. Most of these are off-patent. Relatively affordable generic versions are available as well as brand-name ones. They’ve also been on the market long enough that their benefits and risks have been monitored over time.
Uses. Each medication is most commonly used for a particular set of illnesses based on formal and informal clinical experiences. There are two important caveats. First, just because an illness is on the list doesn’t mean that the medication will help you with that illness. Second, even if an illness is not on the list, the medication may help you with that illness.
Approvals. You’ve likely heard the terms approved for or indicated for applied to medications. These mean that a pharmaceutical company has supplied acceptable evidence to a government regulator (e.g., the FDA or Health Canada) showing that the medication can help with the given problem. Often this evidence comes from clinical trials carried out by the pharmaceutical company. These usually involve at least several hundred patients and take place before the medication is approved in a country.
Not every use for a medication is officially government-approved. Many medications have shown to be very useful for conditions other than those approved by government regulators. Such use is termed off-label. Using a medication off-label is not wrong. Yes, there may be little evidence suggesting it will work. But, there could be strong evidence saying it is helpful, but nobody went through the time-consuming and expensive process of getting government approval. Ask why it’s being recommended in your case.
Approvals also vary by country—we’ll note official approvals in Canada and the USA. Sometimes only one version of a medication is approved even though it comes in multiple forms (usually the newest one the pharmaceutical company is actively marketing). We’ll note this with a ‘†’.
Actions. We note the main neurotransmitters that each medication affects. This only begins to tell the story. Medications act on those neurotransmitters and their receptors in many different ways. Most also have additional effects on other neurotransmitters not mentioned.
Sources. Product monographs are detailed documents prepared by pharmaceutical companies. They are required by regulators (e.g., Health Canada, FDA) and can be considered the official story.
When it comes to combining evidence-based data and real-world use, we have generally deferred to Stahl’s Essential Psychopharmacology: Prescriber’s Guide (sixth edition) by Dr. Stephen Stahl.
The first category of medications is antidepressants. As you’ll recall, these help with not only depression and anxiety but a range of other concerns including impulsivity, skin picking, chronic pain, premature ejaculation, and gastrointestinal distress due to irritable bowel syndrome.
Fluoxetine was the first of the “new generation” of antidepressants to reach the mainstream market (in 1987) and is still in common use today.
Fluoxetine has the longest half-life of current generation antidepressants. After stopping it, it takes up to seven weeks to leave your system, whereas most take two weeks. This leads to minimal withdrawal if any. It’s suitable for people who sometimes miss medication doses. It’s also often prescribed to reduce withdrawal symptoms when tapering off other antidepressants.
It’s most commonly available in capsule and liquid form. Most people find it stimulating, and therefore take it in the morning.
Paroxetine is often used to treat depression in those who also have anxiety. Side effects like weight gain and sedation can be experienced more frequently than with other SSRIs. Paroxetine is associated with significant withdrawal symptoms. Questions regarding its safety in pregnancy (possible increased risk of cardiovascular malformation) are being explored.
Citalopram is generally well tolerated and has relatively few medication interactions. Because of this, it is well-studied and frequently used in people with physical illness taking several other medications. Doses above 40mg carry an increased risk of lengthening the heart’s QTc interval. Escitalopram is very similar to citalopram.
Escitalopram is a newer (went generic in 2012) and cleaner version of citalopram, which was itself already a well-tolerated medication with few interactions. Escitalopram improves on both of these aspects, with an even lower incidence of most side effects and even fewer medication interactions. A dose of escitalopram is equivalent to twice that dose of citalopram. Monitoring the heart’s QTc interval is needed above 20mg, though the medication can be used up to 40mg in most cases.
Despite their similarities, some people find that either citalopram or escitalopram is effective and well-tolerated, but not the other.
Sertraline is another well-studied, well-tolerated medication with few interactions. Notably, it was found to be safe in studies of patients with cardiovascular disease. Sertraline is absorbed 25% better when taken with food.
Fluvoxamine is used for depression and anxiety. It is especially effective in treating obsessive-compulsive disorder (OCD), second only to clomipramine.
It has a low incidence of sexual side effects, though it can cause nausea. It has more potential medication interactions than many other SSRIs. Smoking slows its removal through the liver by 25%, thereby increasing its blood level.
For most people, venlafaxine primarily affects serotonin at lower doses. From 150mg upwards, it affects both serotonin and norepinephrine, and from 225mg upwards, there is a small dopamine contribution.
Above 150mg, it targets symptoms like concentration, motivation, and energy that do not respond as well to SSRIs. It can have a severe discontinuation syndrome, emphasizing the need to stop it very slowly and gradually, in collaboration with your doctor.
While an immediate-release version was first introduced, today, the once-daily extended-release form is used almost exclusively. Venlafaxine can cause hypertension.
Desvenlafaxine is the “next generation” of venlafaxine. Venlafaxine is metabolized into desvenlafaxine by the liver. This newer medication skips this step, so it is not influenced by the CYP450 system or liver disease.
Dosing options (50mg or 100mg tablets) are limited, and the tablets cannot be split without affecting the continuous release mechanism. The 50mg dose affects both serotonin and norepinephrine. Doses above 100mg generally provide little added symptom relief, though side effects increase.
As with venlafaxine, withdrawal symptoms can be severe. If you have problems reducing below the lowest dose of 50mg, you can switch to venlafaxine (desvenlafaxine 50mg ≈ venlafaxine 150mg), which can be reduced more gradually. Alternatively, short-acting low dose desvenlafaxine can be compounded and taken twice daily. Fluoxetine can also be added to decrease withdrawal symptoms.
Duloxetine generally has a lower incidence of problematic side effects and withdrawal symptoms than venlafaxine (the other main SNRI).
Duloxetine works on both serotonin and norepinephrine at the 30mg dose. Doses above 60mg show a greater incremental effect on norepinephrine and dopamine. Dose options are limited in Canada (30mg, 60mg), though a 20mg option is also available in the USA.
For more flexibility, doses of any size can be halved by opening up the capsule and splitting the enteric-coated pellets between the halves. Each half is then sealed, e.g., with a bit of bread or soft cheese. Alternatively, half of the pellets can be added to applesauce, which has the correct pH to maintain the extended-release properties.
The medications we’ve described so far work by inhibiting neurotransmitter reuptake. In contrast, mirtazapine uses a novel mechanism to influence various neurotransmitter receptors. This leads to an increase in serotonin and norepinephrine.
It often helps insomnia and anxiety more quickly than other antidepressants, and its effect can be slightly faster than SSRIs on depressive symptoms. Unlike the SSRIs and SNRIs, it generally does not cause sexual side effects.
Increased appetite leading to weight gain is frequent. Mirtazapine helps those experiencing brain induced nausea due to anxiety or physical illness. It uses the same mechanism as ondansetron, an anti-nausea medication commonly given alongside chemotherapy. Flu-like symptoms (indicating a decreased white blood count), hypotension, and sedation can also occur.
Bupropion is the first medication we’re describing that works on norepinephrine and dopamine, but not serotonin. Most people use the once-daily extended-release version, as opposed to the immediate (three times a day) or sustained (twice a day) version. The latter is used most commonly to change dosages.
Bupropion is frequently added to an SSRI to help with antidepressant-induced sexual dysfunction, as well as provide other benefits. It treats cognitive symptoms of depression, as well as apathy. Bupropion has a lower likelihood than SSRIs of inducing hypomania or mania if a bipolar disorder is suspected.
It will often increase anxiety and irritability, more commonly than the other antidepressants we’ve described so far. Bupropion has a small risk of inducing a seizure (0.4% versus ≤0.1% for SSRIs/SNRIs) and this risk increases to 4% at doses over 450mg. It should not be used if alcohol abuse or withdrawal is an issue, if you’ve had an eating disorder, or if you’re already at risk for seizure.
Bupropion is the same medication marketed as Zyban for smoking cessation.
Amitriptyline is one of the most popular tricyclics, which are the generation of antidepressants that immediately preceded today’s SSRIs and others. It is still widely used, both for severe or treatment-resistant depression and for a variety of chronic physical conditions. Amitriptyline is metabolized into nortriptyline.
When taking a tricyclic, tell your doctor about all of your health conditions, prescribed medications, and supplements. Severe interactions with other medications and natural supplements can occur. Tricyclics can worsen some cardiac and other physical health conditions. They are not safe in pregnancy.
Another tricyclic, your body converts amitriptyline into nortriptyline. The two medications are very similar, both used for treatment-resistant depression and chronic pain. Nortriptyline can be combined with an SSRI to improve cognitive symptoms and apathy. Medication levels can be monitored through simple blood tests, which can help optimize your dosage. It is usually better tolerated than amitriptyline.
See the previous note on amitriptyline regarding tricyclics, medication interactions, and safety.
Clomipramine is a tricyclic antidepressant used for OCD, and to a lesser degree, severe depression. Clomipramine is considered the “gold standard” (most effective) treatment for OCD. However, SSRIs are often tried first because they generally have fewer side effects. Like nortriptyline, its level can be monitored with blood tests to help optimize the dose.
We have included three of the older tricyclic antidepressants that are in common use. There are several others available that are often used in specific situations.
Another broad category of antidepressants is monoamine oxidase inhibitors (MAOIs), whose period of peak use overlapped tricyclics. MAOIs like phenelzine (Nardil) and tranylcypromine (Parnate) are used today, usually when other medications have failed. Most (but not all) require being on a low tyramine diet to prevent a hypertensive crisis. This makes them less appealing to most people.
A few newer antidepressants have been released in recent years. Vilazodone (Viibryd) works on serotonin using a different mechanism than existing medications. Vortioxetine (Trintellix) takes a different approach by targeting multiple neurotransmitters, though can cause severe nausea. Finally, levomilnacipran (Fetzima) is a new SNRI, the same class as venlafaxine or duloxetine. All of these new medications are approved for treating depression. They are used for other illnesses as well.
Other classes of medications are often used to augment antidepressants, helping to address particular symptoms, or boosting the effectiveness of the antidepressant. These include mood stabilizers, sedatives and hypnotics, antipsychotics and stimulants—in other words, everything else!
The next category of psychotropic medications is sedatives (which help reduce anxiety) and hypnotics (which help with sleep). Most of these medications (e.g., benzodiazepines) can help on a short-term or “as needed” basis. As you’ll recall from the Other Medications chapter, they are not used long term as they can affect memory, balance, and reaction time. They are associated with tolerance and withdrawal. For longer-term control of anxiety, other medications (e.g., antidepressants or antipsychotics) are preferred.
Alprazolam is one of the most commonly used anxiolytics, particularly in the USA. It works within 15-30mins, but the effect only lasts a few hours. This makes it a good “as needed” medication. For continuous anxiety, it should be taken at least three times a day, sometimes more, to prevent withdrawal between doses. Withdrawal can cause increased anxiety, called rebound anxiety. A longer-acting, extended-release (XR) version of alprazolam is also available in the USA.
Lorazepam is another short-acting benzodiazepine, which has a fairly wide variety of uses beyond its main use of treating acute anxiety. It’s more commonly used for episodic anxiety in Canada than in the USA, where alprazolam is more popular. Oral, sublingual, intramuscular and intravenous forms are available. It also takes effect quickly, and only lasts several hours, making it a good “as needed” medication. It, too, requires multiple daily doses for ongoing anxiety.
Clonazepam lasts approximately six hours. This is considerably longer than either alprazolam or lorazepam. This makes it a good fit for ongoing anxiety, where using shorter-acting medications may lead to withdrawal and increased anxiety before the next dose. It is also used to help you fall and stay asleep.
Diazepam stays working in your system for several days, and so is very forgiving around the timing of dosages. It, too, is useful for extended periods of anxiety. If you are having difficulty withdrawing from other benzodiazepines, the preferred approach is to switch to diazepam and slowly reduce its dose (see Dr. Ashton’s benzo website, benzo.org.uk). Diazepam is available in pill and intravenous forms.
Zolpidem and other “z-drugs” work similarly to benzodiazepines but are considered somewhat safer. They are still intended for short term use. Short- and long-acting versions of zolpidem are available. Some people report periods of amnesia between when they take the medication and when they fall asleep. Sleepwalking and other behaviours have occurred.
Zopiclone has very similar properties to zolpidem, described previously. Zopiclone is not commercially available in the United States, though the very similar eszopiclone is.
Eszopiclone has very similar properties to zolpidem and zopiclone. Eszopiclone is such a close relative of zopiclone that some jurisdictions denied it patent protection as a unique medication. It is available in the United States. Though short-term use is recommended, technically, the FDA has approved it for longer-term use.
Technically an antidepressant, trazodone is rarely used for depression, as most people cannot tolerate its side effects at the high dose needed to improve depressive symptoms. It’s most commonly used to help fall and stay asleep, though it should be avoided if a bipolar disorder is suspected. Assuming a sufficient dose, it will help with insomnia right away. It’s an excellent alternative to more addictive hypnotics, as there is no development of tolerance, dependence, and limited withdrawal. It can be used over the long term. Postural hypotension can occur. Priapism (prolonged penile/clitoral erection) is a very rare side effect.
Buspirone is often combined with other medications to help with anxiety over the long term. While not a first-line agent, it has a favourable side-effect profile compared with most antidepressants and benzodiazepines. It does take a few weeks to have an effect. It is used either regularly or as-needed to mitigate the sexual side effects of antidepressants.
Pregabalin, and its predecessor, gabapentin, are structurally similar to the neurotransmitter GABA and can cross the blood-brain barrier. Despite that, they don’t actually affect GABA transmission but rely on a different mechanism altogether. Pregabalin can help with pain, as well as both psychological and physical symptoms of anxiety. It has approval in Europe for treating generalized anxiety disorder. Its effects are often felt in one week, faster than antidepressants, and it can be used long term. However, concerns about its abuse potential are beginning to surface. It has a favourable side-effect profile and a wide range of effective doses.
While propranolol is primarily used to reduce blood pressure, it has a few very particular mental health benefits. It can help reduce symptoms of aggression and agitation and is used to decrease performance anxiety. It can reduce feelings of anger and being on edge associated with prior traumatic events, such as those associated with PTSD. It should be used carefully, as it can theoretically worsen depression and cause many physical effects.
Prazosin is another blood pressure medication. It can help reduce nightmares, particularly those associated with posttraumatic stress disorder.
Mood stabilizers are generally a core component of the medication regime used to treat bipolar disorders.
One of the oldest and (chemically) simplest agents, lithium treats acute episodes of mania and depression and helps prevent further high or low mood states. It also significantly reduces suicidal thoughts. It is often paired with one of the anticonvulsant mood stabilizers, an antipsychotic, or (with caution) an antidepressant.
While effective, you need lab tests before starting and periodic lab tests while taking it. Avoiding dehydration and watching for signs of lithium toxicity are also necessary. The correct dosage is determined by blood levels, which can also be affected by other medications. Weight gain and sedation are also common. It is excreted by the kidney and does not depend on the liver at all. It is associated with mild–severe fetal cardiac abnormalities in pregnancy.
Many different formulations of this anticonvulsant are available. It is commonly used in those with bipolar disorders, assisting to keep manic symptoms in check. It can help with aggression, agitation, and impulsivity in other situations. You will need lab tests before starting it, more tests to find the right dosage, and then periodic tests to watch for early signs of long-term physical effects. Weight gain and sedation are common. It can cause fetal neural tube defects in pregnancy, though a folic acid supplement can reduce this risk.
Carbamazepine was the first anticonvulsant widely used to treat bipolar disorders. It also requires lab tests before starting, more tests to find the right dosage, and periodic monitoring for physical effects thereafter. Weight gain is slightly less problematic than with lithium or valproic acid. It is very sedating. It decreases the effectiveness of hormonal contraception. It can cause fetal neural tube defects in pregnancy, though a folic acid supplement can reduce this risk. There is a rare chance of experiencing a severe rash (see lamotrigine, next).
Extended-release versions (e.g., Tegretol CR) and a successor medication, oxcarbazepine (Trileptal) are overall better tolerated by many people.
Compared to lithium, valproic acid, and carbamazepine, lamotrigine is very well tolerated. It has a lower incidence of side effects and little tendency toward weight gain or sedation. Lab tests are not required either before or during use, though its blood level is decreased with hormonal contraception. It is more effective in treating acute depressive symptoms, so is used for bipolar depression and less commonly for unipolar depression with anxiety.
There is a rare possibility (BODYlt;0.1%) of developing a rash that, if left untreated, can become very serious and even life-threatening called Stevens-Johnson Syndrome (SJS). However, around 10% of people taking lamotrigine develop a benign rash. Slower and smaller dose changes decrease the risk of developing a rash. It is important to monitor yourself for a rash, especially around dose changes, and see your doctor if one occurs. Most times, the rash disappears once the medication is discontinued.
These medications are used at higher doses to treat schizophrenia, severe bipolar disorders, and other psychoses. They are increasingly used at lower doses, in combination with an antidepressant, to manage anxiety and unipolar depression. The antipsychotics included here are considered “atypical” antipsychotics, as compared with the first generation of antipsychotic medications, e.g., Haldol.
Typically used at higher doses to address psychosis, at lower doses, it is often used to help with overall mood stability, aggression, anxiety and insomnia. It can help prevent nightmares in PTSD. Unlike many sedatives and hypnotics, it is not addictive, so it can be used long term if needed. It can be associated with metabolic syndrome (e.g., weight gain, increased cholesterol, diabetes), especially at higher doses. Initial metabolic testing and periodic monitoring are warranted. Immediate and extended-release formulations are available.
Like quetiapine, it is used at higher doses for psychosis and lower doses for overall mood stability, aggression, and agitation. It is less sedating than quetiapine. Unlike many sedatives and hypnotics, it is not addictive, so it can be used long term if needed.
Metabolic syndrome is again a concern, so initial metabolic testing and periodic monitoring are warranted. Below 6mg, most people experience less weight gain on risperidone than quetiapine or olanzapine. Above 6mg, side effects commonly seen with typical antipsychotics can occur, e.g., parkinsonism. It can cause elevated prolactin levels in some people, possibly causing breast tenderness and lactation. Long term, increased prolactin can cause osteoporosis, so it is important to report these symptoms to your doctor.
Like risperidone, it is used at higher doses for psychosis and lower doses for overall mood stability, anxiety, aggression, and agitation. It is also often used to augment other medications when treating unipolar or bipolar depression. It can be used long term if needed. It is fairly sedating. Many people experience significant weight gain and metabolic syndrome. Initial metabolic testing and periodic monitoring are warranted.
Lurasidone is one of the better-tolerated antipsychotics, used for similar purposes. It does not usually cause weight gain over the long term, though it is often somewhat sedating. Unlike some of the other medications, it can be taken once a day but needs to be taken with at least 350 calories of food.
Aripiprazole is not as frequently associated with either weight gain or sedation. At lower doses (1-5mg), it is often used to augment antidepressants (“augment with Abilify!” proclaims the advertising). Some people find it activating. This can help with symptoms of depression like anhedonia and fatigue. It also treats cognitive symptoms. Watch for feelings of inner motor restlessness. A successor medication, brexpiprazole (Rexulti) is also now available.
This section includes medications for ADHD. These medications are also used to augment antidepressants to improve concentration, fatigue, and inattention due to other causes like depression.
The most common agents are stimulants based on either amphetamine or methylphenidate. Some non-stimulant medications in this category are also available that don’t have the same abuse potential.
Amphetamine-based psychostimulants are primarily used to treat ADHD, and often as an augmenting agent to improve cognitive symptoms of depression. Lisdexamfetamine (Vyvanse) is the only one approved for binge eating disorder.
Because they use different delivery mechanisms, the length of time they work varies. Overall, they start working quickly. Their effect peaks within an hour or two, then gradually tails off. For example:
Dexedrine (one peak, lasts ~4h)
Dexedrine spansules (one peak, lasts ~6-8h)
Adderall XR (one peak, lasts ~12h)
Vyvanse (one peak, then fairly level, lasts ~13-14h)
The other main psychostimulant medications are those made of methylphenidate. As with the amphetamine-based medications, a variety of delivery mechanisms are used which provide different durations and patterns of effect. Most start working quickly, their effect peaking within an hour or two, and then gradually tail off. Some have a second peak, a few hours after the first, as if you’d taken a second dose. For example:
Ritalin (one peak, lasts ~3-4h)
Ritalin LA (two peaks, lasts ~6-8h)
Concerta (one peak, lasts ~12h)
Aptensio/Biphentin (two peaks, lasts ~10-12h)
Atomoxetine is a non-stimulant medication for the treatment of ADHD, which does not have abuse potential like the amphetamine- and methylphenidate-based medications. Those with bipolar disorders should watch for the possible development of a hypomanic or manic episode.
Several other medications are commonly used for symptoms of ADHD, fatigue, concentration, etc. Guanfacine (Intuniv) is a blood pressure medication that has also been approved for ADHD. Like atomoxetine, it also has no known abuse potential. Clonidine is another blood pressure medication with similar properties. Modafinil (Alertec), another low-abuse alternative to stimulants, is approved to treat excessive sleepiness in narcolepsy, shift workers, sleep apnea, and fatigue due to other physical illness. It also helps improve attention in ADHD and fatigue. The antidepressant bupropion (Wellbutrin) can also provide some help for these symptoms.
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