Pharmacho therapy and Psychopharmacology Note

Therapeutic Techniqes:PSM-415 Saturday, May 20, 2017
1 | P a g e Geetesh Kumar Singh, M.A.-IV SEM, Department of Psychology, DAV PG College (BHU), Varanasi - 221001 E-mail: g_ksingh007@yahoo.com
PSYCHOPHARMACOLOGICAL THERAPY
Psychopharmacology is the scientific study of the effects of drugs on mood, sensation, thinking and behavior.
According to Chaplin (1975)- Psychopharmacology refers to the use of drugs in the treatment of mental disorder.
According to Rebber (1987)- Psychopharmacology refers to any forms of psychotherapy that treats behavioral and
mental disorders with the help of drugs and chemicals.
Actually psychopharmacology is the science of determining which drugs alleviate which disorders and why they do
so. The drugs which is used for the treatment of mental disorder is called psychoactive drugs or psychotropic drugs.
Psychoactive drugs/Psychotropic drugs interact with particular target sites or receptors found in nervous system
to induce widespread change in physiological or psychological functions.
Psychotropic medication: Medications that affects psychic function, behavior or experience
Neurotransmitter: A chemical that is stored in the axon terminals of the presynaptic neuron
Receptor: Molecules situated on the cell membrane that are binding sites for neurotransmitters
Drug Action: The specific interaction between drugs and receptors is referred to as “drug action”, (It is also called
Pharamacodynamics).
Drug Effect: The widespread change in physiological or psychological function is referred to as “drug effect”.
Efficacy - Ability of a drug to produce a response as a result of the receptor or receptors being occupied.
Potency - Dose required to produce the desired biologic response.
Loss of effect - desensitization (rapid decrease in drug effect), tolerance (gradual decrease in the effect of a drug at a
given dose), can lead to being treatment refractory.
Pharmacokinetics How the Body Acts on the Drug? 1) Absorption 2) Distribution 3) Metabolism 4) Elimination
1) Absorption is the movement of a drug into the bloodstream. Absorption involves several phases.
Route of Administration: i) Oral ii) Topical Dermal iii) Dosage form (tablet, capsule, or solution) iv) Intravenous
therapy v) Intramuscular injection vi) Eternal nutrition. The fastest route of absorption is inhalation, and not as
mistakenly considered the intravenous administration.
2) Distribution Amount of drug found in various tissues, especially the intended ones. Psychiatric drugs must pass
through blood-brain barrier. Factors effecting distribution are -
i) Size of organ (larger requires more) ii) Blood flow (more, greater concentration) iii) Solubility (greater, more
concentration) iv) Plasma Protein (if bound, slower distribution, stays in body longer) v) Anatomic Barriers (tissues
surrounding)
3) Metabolism Process by which the drug is altered and broken down into smaller substances (metabolites) that are
usually inactive. Lipid-soluble drugs become more water soluble, so they may be more readily excreted. Most
metabolism is carried out in the liver.
4) Elimination
Clearance: Total amount of blood, serum, or plasma from which a drug is completely removed per unit time.
Half-life: Time required for plasma concentrations of the drug to be reduced by 50%.
Only a few drugs eliminated by kidneys (lithium). Most excreted in the liver
– excreted in the bile and delivered to the intestine
– may be reabsorbed in intestine and “re-circulate” (up to 20%)
Concept of Half Life of Drugs
The duration of action of a drug is known as its half-life. This is the period of time required for the concentration or
amount of drug in the body to be reduced by one-half. We usually consider the half-life of a drug in relation to the
amount of the drug in plasma. A drug's plasma half-life depends on how quickly the drug is eliminated from the
plasma. A drug molecule that leaves plasma may have any of several fates. It can be eliminated from the body, or it
can be translocated to another body fluid compartment such as the intracellular fluid or it can be destroyed in the
blood. Both of these pharmacokinetic parameters are important in determining the half-life of a drug. The symbol to
represent the half-life of drug is t½.

Major Categories of Drugs
1- Neuroleptics 2- Anxiolytics 3- Hypnotics 4- Antidepressants
5- Mood Stabilizers 6- Psychostimulants
1. NEUROLEPTICS /ANTIPSYCHOTIC AGENTS
Indications:
– These are also called major tranquilizers and neuroleptics.
– They are used in the treatment of acute and chronic psychoses particularly when accompanied by
increased psychomotor activity.
– Selected agents are used as antiemetics in the treatment of intractable hiccoughs and for the control of
tics and vocal utterances in Tourette’s disorder.
– Antipsychotic drugs are divided in to two categories: Typical Neuroleptics and Atypical Neuroleptic
Antipsychotic Drugs:
Examples of First generation or Conventional
antipsychotics or Typical Neuroleptics:
1-Phenothiazines (Thorazine, Prolixin)
2-Thioxanthene (Navane)
3-Butyrophenones
4- Dibenzoxazepines (Loxitane)
5-Haloperidol (Haldol)
SideEffects: Appeared Movement Related disorders
which is called Extrapyramidal Symptoms.
Examples of Second generation or Novel antipsychotics
or Atypical Neuroleptics:
1-Clozapine (Clozaril)
2-Risperidone (Risperdal)
3-Olanzapine (Zyprexa)
4-Quetiapine (Seroquel)
5-Ziprasidone (Geodon)
Side Effects: A-Positive Side Effects: delusions,
Hallucinations, disorganiged speech and behavior.
B-Negative Side Effects: Flat affect, Poverty of speech,
Loss of directions
Side effects of antipsychotics:
– Anticholinergic
effects such as dry
mouth, blurred
vision, constipation,
urinary retention
– Nausea
– Skin rash
– Sedation
– hypotension
– Photosensitivity
– Hormonal effects
– ECG Changes
– Reduction of seizure
threshold
– Hypersalivation
Extrapyramidal symptoms (EPS): They are related to movement disorder and related to typical Neuroleptics.
1-Pseudoparkinsonism: Rigidity, Tremor in hand and leg, sad facial expression, mask like face, loss of spontaneous
movements and some time show rabbit syndrome. Cognitive symptoms involve impaired thinking ability
2-Akinesia: Slow movement or This is loss of standard motor functions or slowness that causes impaired movement
of muscle and plainly “without movement” or “without much movement”. It can be caused by paralysis, that is
temporary and also from being in a coma. It might disturb all or only a portion of the body.
3-Akathisia: An often distressing sense of inner restlessness or patients typically complain of feeling of restless.
Obvious sign of restlessness includes continual foot-tapping, marching, pacing or shuffling. Patients might also rock
back and forth while sitting or standing. Other symptoms include continually shifting body weight from one leg to
another.
Dystonia: Series of uncontrollable contractions in eye, back, tongue and muscles
Oculogyric crisis: A prolonged involuntary upward deviation of the eyes.
Tardive dyskinesia: Irregular, repetitive involuntary movements of mouth, face, and tongue, including chewing,
tongue protrusion, lip smacking, puckering of the lips, and rapid eye blinking. Abnormal finger movements are
common.
Neuroleptic malignant syndrome: NMS typically consists of muscle rigidity, fever, autonomic instability, and
cognitive changes such as delirium.
Hyperglycemia and diabetes: high blood sugar is a condition in which an excessive amount of glucose circulates in
the blood plasma.
2. ANXIOLYTICS DRUGS
Indications:
o These are also called Antianxiety Agents and minor tranquilizers.
o These are used in the treatment of anxiety disorders, anxiety symptoms, acute alcohol withdrawal,
skeletal muscle spasms, convulsive disorders (an uncontrolled shaking of the body), and sedation.

o These drugs are used to treat people who have a high level or prolonged state of anxiety that is strong
enough to incapacitate them, or at least cause them difficulty in carrying out many activities of daily
life.
Famous Anxiolytics:
Benzodiazepines
• The most important and widely used class of antianxiety drugs. The first Benzodizepines were released in the
early 1960s.
• Gitlin(1996), Roy-Byrne & Cowley (2002) have reported that one problem with this drug is patients can
become psychologically and physiologically dependent on them.
• They also reported that benzodiazepines are enhancing the activity of GABA (gamma aminobutyric acid: It is
an inhibitory neurotransmitter.
Side effects:
- Drowsiness, confusion,
lethargy
- Tolerance
- Physical & psychological
dependence
– Blurred Vision
– Depression and lack
of energy
– Memory loss
– Slow reflexes and
slurred speech
– Impaired thinking
– Nausea & vomiting
Buspirone
• It is completely unrelated to the benzodiazepines and released since the early 1960s.
• Gitlin(1996), Roy-Byrne & Cowley (2002) have cleared that it act in complex ways on serotonergic
functioning rather than on GABA.
• Buspirone relieves anxiety by increasing serotonin in the brian as the SSRI.
• Buspirone is slow drug and it takes about two weeks to start working on Anxiety.
• However it has several advantages over the older anti-anxiety drugs such as:
(i) Withdrawal effects are minimal (ii) Not addictive (iii) Not impair memory and attention
(iv) Not disturb motor co-ordination
3. HYPNOTICS DRUGS
 Hypnotic drugs are regularly prescribed for insomnia and other sleep disorders, with over 95% of insomnia
patients being prescribed hypnotics in some countries.
 Hypnotic or soporific drugs is commonly known as sleeping pills.
 The primary function is to induce sleep and to be used in the treatment of insomnia/sleeplessness or surgical
anesthesia. This group is related to sedatives.
 The term sedative describes drugs that serve to calm or relieve anxiety and the term hypnotic generally
describes drugs whose main purpose is to initiate, sustain, or lengthen sleep.
 Brunton, Laurence Lazo, John, Parker, and Keith (2006) have reported that because these two functions
frequently overlap, and because drugs in this class generally produce dose-dependent effects.
Chemical class Generic
(trade) name
Medication Action on NT/
Receptor
Physiological
effects
Side effects
Benzodiazepines Alprazolam
Librium
Clonazepam
(Klonopin)
Clorazepate
(Traxene)
Diazepam
(Valium)
Lorazepam
(Ativan)
Oxazepam
(Serax)
Antianxiety:
Benzodiazepines
Binds to BZ
receptor sites on
the GABA
receptor complex,
increases receptor
affinity for GABA
Relief of
anxiety
Sedation
Dependency (with
long term use)
Confusion,
memory
impairment,
motor
incoordination
Buspirone (Buspar) Antianxiety:
Buspirone
5-HT agonist
D2 agonist
D2 antagonist
Relief of
anxiety
Nausea, headache,
dizziness
Restlessness

Indications:
 They are used in the short term management of various anxiety states and to treat insomnia.
 Selected agents are used as anticonvulsants and preoperative sedatives and to reduce anxiety associated
with drug withdrawal
 Many hypnotic drugs are habit-forming and disturb the human sleep pattern.
 A physician may suggest changes in the environment before and during sleep.
Category of Hypnotics:
1-Barbiturates: 2-Benzodiazipines: 3-Quinazolinones:
Butabarbital, Mephobarbita Estazolam, Quazepam Cloroqualone, Diproqualone
Barbiturates
• Barbiturates are drugs that act as central nervous system depressants.
• And they can produce a wide spectrum of effects: (i) Mild sedation (ii) Total anesthesia.
Benzodiazepines
• It can be useful for short-term treatment of insomnia.
• Their use beyond 2 to 4 weeks is not recommended due to the risk of dependence.
• It is preferred that benzodiazepines be taken intermittently and at the lowest effective dose.
• They improve sleep-related problems by shortening the time spent in bed before falling asleep, prolonging the
sleep time, and, in general, reducing wakefulness
Quinazolinones
 Quinazolinones are also a class of drugs which function as hypnotic/sedatives.
 Their use has also been proposed in the treatment of cancer.
Side Effects of Hypnotics/Sedative:
• Burning or tingling in the
hands, arms, feet, or legs
• Changes in appetite
• Constipation
• Diarrhea
• Difficulty keeping balance
• Dizziness
• Daytime drowsiness
• Dry mouth or throat
• Gas
• Headache
• Heartburn
• Impairment the next day
• Mental slowing or problems
with attention or memory
• Stomach pain or tenderness
• Uncontrollable shaking of a
part of the body
• Unusual dreams
• Weakness
4. ANTIDEPRESSANTS DRUGS
Indications:
– It is used in the treatment of sleep disorder, major depression, snoring, eating disorder, anxiety
disorder, alcoholism, schizophrenia or mental retardation, depressive phase of bipolar disorder and
depression accompanied by anxiety.
– These drugs elevate mood and alleviate other symptoms associated with moderate-to-severe
depression
– Antidepressants reduce symptoms of mood disorders primarily through the regulation of
norepinephrine and serotonin.
– Antidepressants can be used alone or in the combination with other medicines.
– Most antidepressants block the re-uptake of a neurotransmitter of one or more of the bioamines:
serotonin, norepinephrine, dopamine.
– The most important classes of antidepressants are the selective serotonin reuptake inhibitors
(SSRIs), tricyclic antidepressants (TCAs), monoamine oxidase inhibitors (MAOIs).
Some Important Antidepressants:
Chemical
class
Generic (trade) name
TCAs Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline,
Protriptyline, Trimipramine
SSRI’s Citralopram, Fluoxetine, Fluvoxamine, Escitalopram, Paroxetine, Sertraline
MAOI Isocarboxazid, Phenelzine, Tranylcypromine
Others Bupropion, Maprotiline, Mirtazapine, Trazodone, Nefazodone, Venlafaxine, Duloxetine

Effects of Antidepressants on neurotransmitters:
Medication Action on NT/ Receptor Physiological
effects
Side effects
TCAs  Inhibit reuptake of serotonin
 Inhibit reuptake of
norepinephrine(NE)
 Block NE receptor
 Block Ach receptor
 Block histamine receptor
 Reduce
depression
 Relief of
severe pain
 Prevent
panic
attacks
Sexual dysfunction
Sedation, weight gain
Dry mouth, constipation, blurred
vision, Constipation, Urinary
retention, hypotension,
Photosensitivity, Weight gain
SSRI’s Inhibit reuptake of serotonin  Reduce
depression
 Control
anxiety
 Control
obsessions
Nausea, agitation, headache, sexual
dysfunction, Insomnia, Irritability,
Fatigue, Agitation, Weight loss,
Electric shock sensation, Fetal
Prematurity
MAOI Increase NE by inhibiting the enzyme
that degrades them. Increases levels of
NE and Serotonin in CNS
 Reduce
depression
 Control
anxiety
Sedation, dizziness, Sexual
dysfunction, Hypertensive crisis,
Headache, High blood Pressure,
REM REBOUND*
*In which the patient experiences extremely vivid dreams and nightmares
5. MOOD STABILIZING AGENTS
 Mood stabilizers are medicines used in the treatment of bipolar disorder.
 These drugs can help reduce mood swings and prevent manic and depressive episodes.
 More recently, the concept of "mood stabilizer" has been defined in a wide-ranging manner to treat bipolar
disorder.
Indication:
 Atypical antipsychotic used to treat “bipolar disorder," with antidepressants being considered as mood
destabilizers.
 With all this competing terminology and the number of drugs for the treatment of bipolar disorder exploding,
the term "mood stabilizer" has become so confusing that regulatory authorities and some experts.
 They suggest that it would be best to use another term for agents that treat bipolar disorder.
 Rather than using the term “Mood stabilizers," some would argue that there are drugs that can treat any or
all of four distinct phases of bipolar disorder.
 Thus, a drug can be “Mania-minded" and "treat from above" to reduce symptoms of mania and/or "stabilize
from above" to prevent relapse and the recurrence of mania.
 Furthermore, drugs can be “Depression-minded" and "treat from below" to reduce symptoms of bipolar
depression and/or "stabilize from below" to prevent relapse and the recurrence of depression
Drugs Related to Mood Stabilizers:
Chemical class Generic (trade) name Uses
Antimanic Lithium carbonate (Camcolit,
Liskonum, Priadel, Lithonate, Litarex)
Prevention and treatment of manic episodes of
bipolar disorder, alcohol dependence, major
depression
Anticonvulsants Clonazepam, Carbamazepine, Valporic
acid, lamotrigine, gabapentin, topiramate
All stages of seizures
Calcium channel
blocker
Verapamil hypertension, bipolar mania, migraine headache
Antipsychotics Olanzapine, aripiprazole,
chlorpromazine, quetiapine, risperidone,
ziprasidone
Schizophrenia, bipolar mania

Side Effects:
Antimanic Anticonvulsants Calcium channel
blocker
Antipsychotics
Drowsiness, dizziness,
headache, Dry mouth,
thirst, Nausea/
vomiting, Fine hand
tremors, Hypotension,
Pulse irregularities,
Dehydration, Weight
gain
Drowsiness, dizziness, headache, Dry
mouth, thirst, Nausea/ vomiting, Fine
hand tremors, Hypotension, Pulse
irregularities, Dehydration, Weight
gain Weight gain, Alopecia (hair loss),
Blood dyscrasias, Risk of severe rash,
Decreased efficacy, Minimized by
treating in low doses & Give with food
Drowsiness,
Dizziness
Hypotension,
Bradycardia
(abnormally slow
heart rate),
Nausea,
Constipation
Drowsiness, Dizziness,
Dry mouth, Constipation,
Increased appetite,
Weight gain, ECG
changes, Extra Pyramidal
Symptoms,
Hyperglycemia &
diabetes
6. PSYCHOSTIMULANTS DRUGS
• A psychostimulant is a drug that produces a temporary increase in psychomotor activity or a temporary
improvement in physical functions or mental processes or both.
• A psychomotor activity is one that involves the coordination of motor skills with thought; for example,
throwing a baseball, brushing our teeth, etc.
• Psychostimulants are drugs that can improve our ability both physically and mentally during such activities.
• The most commonly used psychostimulants are caffeine, nicotine, amphetamines, methamphetamine,
Ecstasy, cocaine and methylphenidate.
• Stimulants have been used in medicine for many conditions including: Obesity, Sleep Disorder, Mood
Disorder, Impulse Control, Asthma, Nasal Congestion, Anesthetics
Indication:
• Drugs used to treat obesity are called Anorectics.
• Drugs used to treat sleep disorders such as excessive daytime sleepiness are called eugeroics.
• Stimulants are used in impulse control disorders such as ADHD and off label in mood disorders such
as Major Depressive Disorder to increase energy, focus and elevate mood.
• Psychostimulants are also called stimulants.
• They mainly consist of amphetamines (Dexedrine) and methylphenidates (Ritalin, Metadate and
Methylin), which are very similar in chemical structure to amphetamines.
• A stimulant refers to any mind-altering chemical or substance that affects the central nervous system
by speeding up the body’s functions, including the heart and breathing rates.
General Effects of Psychomotor Stimulants
• Increase in behavioral and motor activity
• Increase in alertness and disruption of sleep
• Pupil dilation, shift in blood flow from skin and organs to muscle, increased body temp.
• Increase in blood pressure and heart rate
• Increased O2 and glucose levels in the blood
• Side effects of anxiety, insomnia and irritability
• Effects synaptic action of dopamine, serotonin & norepinephrine
Amphetamine or Dexedrine Pharmacological Effects
• First produced in 1937, used in WWII by Germans, British and Japanese. United States started using
amphetamine during the Korean War.
• Response intensity and duration varies at the type of drug, dose & route of administration
• Low dose: typical psychomotor stimulation
• Moderate dose: tremors, insomnia, agitation, increased respiration
• Continuous high doses: repetitive activity, aggression, delusions, anorexia
• Detectable in urine for 48 hours
Non-Amphetamine Behavioral Stimulants Methylphenidate or Ritalin
• Used in treatment of ADHD to calm hyperactivity and improve attention (prescribed in 90% of cases)
• Half-life ≈ 2-4 hours

• Variable absorption rates, but generally a rapid onset with short duration (multiple administrations needed
over the course of a day)
• Increase attention, Increase inhibition (improve brake linings on the brain).
• Reduce hyperactivity
• Acts the same in adults.
• Small dose helps concentration, alertness.
• Higher doses become too hyper, lose concentration.
Side Effects of Psychostimulants:
--Abdominal pain
– Aggression
– Angina (sudden chest pain)
– Anorexia (eating disorder)
– Blood pressure and pulse changes
– Blurred vision
– Depression
– Dizziness
–Drowsiness
– Dry mouth
– Fever
– Hallucinations
– Headaches
– Heart palpitations
– Hypersensitivity
– Increased irritability
– Insomnia
–Involuntary tics and twitching
called Tourette’s syndrome
– liver problems & loss of appetite
--Mental/mood changes
– Moodiness & nausea
– Nervousness
– Psychosis
– Restlessness & Seizures
– Suicidal thoughts
– Unusual weakness or tiredness
– Violent behavior
– Vomiting
– Weight loss

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