Antidepressants, Psychomotor Stimulants, and Lithium

Selective Serotonin Reuptake Inhibitors (SSRI)

A group of drugs that have a very selective action to block the reuptake of serotonin (5HT) back into the serotonergic nerve endings. This action increases the concentration of 5HT in the synaptic cleft, which results in increased stimulation of serotonin receptors

Which TCAs have a high degree in sedation?

Clomipramine, Doxepin, Amitriptyline

MAOI adverse effects

Common dry mouth urinary retention, constipation, blurred vision, hypotension, weight gain, and sexual dysfunction CNS disturbances include restlessness, dizziness, insomnia, tremors, and seizures. Liver damage may be fatal

SSRI overdose

Confusion, fever, tremor agitation, restlessness, and other signs of CNS excitation. Seizures have also been reported. May lead to coma and death if not treated.

Lithium pregnancy category

D

SSRI discontinuation

Dizziness, nausea, insomnia, and anxiety. Dosage should be reduced over time

Lithium occasionally produces disturbances in the ________ gland. Patients with preexisting condition should not take

thyroid

The daily dose of Prozac, or Fluvaxamine, should be

20-60 mg

Desvenlafaxine

Active metabolite of venlafaxine and has similar properties

Trycyclic adverse effects

Anticholinergic effects include dry mouth, constipation, urinary retention, and rapid heartbeat. Alpha-blocking actions may cause postural hypotension, blurred vision, and drowsiness. CNS stimulation may produce restlessness, tremors, convulsions, or mania

Serotonin-norepinephrine Reuptake Inhibitors

Block reuptake of serotonin like the SSRIs and also block the reuptake of norepinephrine to increase the levels of both serotonin and norepinephrine in the brain Like the SSRIs, they have little effect in blocking cholinergic, adrenergic, or histamine receptors

Major Depressive Disorder

Depression that arises from within an individual and requires psychotherapy and treatment. Psychological disturbances and maladjustments or biochemical defects in the brain are thought to be involved

Exogenous, reactive depression

Depression that is caused by external factors (death or unemployment). Self-limiting and usually does not require drug therapy. The love and understanding of family or friends support the individual through the crisis

Venlafaxine (Effexor), desvenlafaxine (Pristiq), and duloxetine (Cymbalta)

Drugs that block the reuptake of both serotonin and norepinephrine

MAO inhibitors (MAOIs)

Drugs that inhibit, or block MAO.

SSRI clinical indication

Effective in the treatment of major depression and most anxiety disorders such as post traumatic stress disorder (PTSD) and obsessive-compulsive disorder (OCD). In OCD, individuals have repetitive and excessive impulses to perform some physical or behavioral action. These impulses can interfere with and disrupt the normal daily routine of work and living.

Monoamine oxidase (MAO)

Enzyme that inactivates norepinephrine an serotonin excreted by kidneys. Found in most body cells but particularly in the adrenergic and serotonergic nerve ending.

Fluoxetine

Fluoxetine was the first SSRI to be introduced

Which drugs are also indicated in the treatment of OCD?

Fluoxetine, Paroxetine, Zoloft, and Prozac

MAOI dietary restrictions

Foods that normally contain tyramine include wine, beer, herring, and certain cheeses. In addition, certain sympathetic drugs used in the treatment of cold symptoms (decongestants and bronchodilators) interact with the MAO inhibitors, causing potentiation of the effects of the sympathetic agents

SSRI adverse effects

GI disturbances including nausea, dry mouth, and anorexia CNS effects include headache, nervousness, insomnia, and tremors Reduced sexual interest and delayed orgasm

Duloxetine

Generally causes low incidence of CNS activation

Drugs used to treat depression

Known as antidepressants, or mood elevators. Increase levels of norepinephrine (NE) and serotoin (5HT)

Mood stabilizers

LIthium, Carbamazepine, Lamotrigine, Valproate

LIthium toxicity

Lithium and sodium ions compete with each other for renal elimination. Adequate sodium intake is necessary for proper urinary excretion of lithium. Decreased sodium intake and hyponatremia (low sodium levels) promote the retention of lithium

Lithium pharmacokinetics

Lithium is administered as a salt, lithium carbonate, in the form of capsules (Eskalith) or controlled release and slow-release tablets (Eskalith CR, Lithobid). Usually 1 to 2 weeks of treatment are required before therapeutic effects are observed.

Tyramine

Many foods contain a substance known as tyramine, which causes the release of norepinephrine from storage granules located inside the adrenergic nerve endings. When MAO is inhibited, tyramine may produce a massive release of norepinephrine, which can result in serious consequences, such as hypertensive crisis or cerebral stroke

Depression

Mental state characterized by depressed mood, with feelings of frustration and hopelessness

Mania

Mental state of excitement, hyperactivity, and excessive elevation of mood

Venlafaxine

Moderately activating and has adverse effects similar to the SSRIs. Increases in diastolic blood pressure are evident at higher doses.

Bipolar mood disorder

Mood disorder where episodes of mania and depression occur alternatively

LIthium fatal overdose

Muscle fasciculations, convulsions, and circulatory collapse lead to death

Amphetamines act on which two neurotransmitters?

Norepinephrine and dopamine

SSRI drugs

Paxil, Zoloft, Luvox

Trycyclic pharmacological actions

Produce varying degrees of sedation, anticholinergic effects, alpha-adrenergic blockade, and antihistaminic effects. Degree of sedation, anticholinergic, and alpha-blocking effects among the various drugs

MAOI mechanism of action

Require 2 to 4 weeks to produce their maximum effect. After a week or so of treatment, there is usually an improvement in appetite and sleep, followed by an elevation of mood and an overall improvement in mental state. These effects continue for approximately 2 weeks after termination of treatment

Fluoxetine and sertraline

SSRIs approved for premenstrual dysphoric disorder, where mood disturbances occur in relation to the menstrual cycle

The major antidepressant drug classes include the

Selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), and monoamine oxidase inhibitors (MAOIs)

Lithium adverse effects

Side effects are common, even at therapeutic doses. Initially, most patients experience some nausea or tremors that usually disappear with continued treatment

SNRI adverse effects

Similar to SSRIs. Increased levels of norepinephrine can raise blood pressure, heart rate, and CNS activation. Sudden discontinuation syndrome

SSRI mechanism of action

The increase in 5HT activity in the limbic and cerebral cortical areas of the brain is believed to contribute to the antidepressant effect. Clinical improvement usually requires several weeks to fully develop. The SSRIs usually stimulate and activate CNS activity.

Trycyclic mechanism of action

The pharmacological actions occur within a few hours of administration. However, the full antidepressant effect requires 2 to 4 weeks to develop. Consequently, it is believed that tricyclics and related antidepressant drugs may produce additional pharmacologic actions that are not yet completely understood

Monoamine Theory of Mental Depression

Theory that mental depression is caused by low brain levels of norepinephrine and serotonin (monoamines)

Uses of SNRIs

Treatment of general anxiety, chronic pain disorders, and fibromyalgia

Trycyclic antidepressants

Triple-ring structure. Block the reuptake of norepinephrine and serotonin back into the neuronal nerve endings

Lithium

Used for the treatment of mania and bipolar mood disorder. It is often used in combination with antidepressant drugs in the manic-depressive or bipolar form of psychosis

Lithium overdose

Vomiting, diarrhea, drowsiness, loss of equilibrium, ringing in the ears, and frequent urination are common. At toxic levels, the heart and kidneys may be damaged, leading to the development of cardiac arrhythmias or nephritis

Early recognition and treatment are essential for prevention of the serious consequences of ________

depression

Newer studies suggest that deficiencies of ________ factors and other _______ factors that support brain function may also play a role in mental depression.

endocrine, neurotrophic

Low levels of ______ and/or ______ are associated with mental depression, while high levels of norepinephrine and/or serotonin may be involved in _______

norepinephrine, serotonin mania

Lithium is an element similar in chemical properties to _______. The body utilizes lithium as if it were _____. Both lithium (Li+) and _______ exist in body fluids as charged particles, or ions.

sodium Na+

Certain ________ drugs used in the OTC treatment of colds and seasonal allergies interact with MAOIs

sympathetic