ADRENERGIC AGONISTS AND ANTAGONIST

Opposite response

Sympathomimetic + Parasympathomimetic =

Opposite response

Sympatholytic + Parasympatholytic =

Similar response

Sympathomimetic + Parasympatholytic =

Similar response

Sympatholytic + Parasympathomimetic

ANS DRUGS (Autonomic Nervous System Drugs)

1. Adrenergic agonist

2. Central Acting Alpha Agonist

3. Adrenergic Antagonists (Adrenergic Blockers)

CATEGORIES OF SYMPATHOMIMETICS

1. Direct-acting

2. Indirect-acting

3. Mixed-acting

ADRENERGIC AGONIST

Mimics the sympathomimetics Norepinephrine and Epinephrine and act on the adrenergic receptors in the effector cells of the ff:

1. Heart

2. Bronchioles

3. GIT

4. Urinary bladder

5. Ciliary muscles of the eye

NON-SELECTIVE ADRENERGIES

1. Norepinephrine

2. Epinephrine

3. Ephedrine

4. Dopamine

SELECTIVE ADRENERGICS

1. Dobutamine

2. Phenylephrine

3. Clonidine

4. Dexmedetomidine

Epinephrine

Emergency medication for anaphylactic reactions

Potent inotropic

is a medication that significantly increases the force of contraction of the heart muscle.This increased contractility can improve the heart's pumping ability, leading to increased blood flow to the body's organs

Phentolamine mesylate

antidote of epinephrine

Albuterol

Relaxation of the smooth muscles of the lungs and uterus

1. Beta 2 adrenergic agonist, selective

2. Onset of action 5-15 via inhalation

Clonidine (CENTRAL-ACTING AGONIST)

is a medication that primarily works by reducing activity in the sympathetic nervous system, which is responsible for the body's "fight or flight" response. Selective alpha 2 agonist: trt for HPN

ADRENERGIC ANTAGONIST

Beta-receptor drugs are drugs that attach to Beta-Adrenergic receptors and block the effects of agonist

1. Prevents cardiac and pulmonary excitation

2. Non-selective or cardioselective

3. Propanolol, metoprolol, esmolol, atenolol, nadolol, pindolol, labetalol, and carvedilol.

ADRENERGIC ANTAGONIST

1. Adrenergic blockers

2. Sympatholytics

3. Blocks alpha and beta

4. Beta-Adrenergic Antagonist (beta blockers)

CHOLINERGIC AGONIST

1. Stimulates the parasympathetic nervous system

2. Cholinergic agonists are parasympathomimetics

3. Anticholinergics are parasympatholytics

4. Stimulate bladder and GIT tone, constrict pupils, increase

   neuromuscular transmission

5. Decrease HR and BP, increases salivatory, GI, bronchial and glandular secretions

6. Metoclopramide hydrochloride (GERD)

7. Pilocarpine (Glaucoma)

8. Atropine sulfate (antidote)

Metoclopramide hydrochloride (GERD)

can be used to treat GERD is a medication primarily used to treat conditions related to delayed gastric emptying and nausea and vomiting. It works by increasing the muscle contractions in the upper digestive tract, which helps to speed up the movement of food from the stomach to the intestines.

Pilocarpine

is a medication used to treat glaucoma, a condition that damages the eye's optic nerve and can lead to vision loss. It works by increasing the drainage of fluid from the eye, which helps to lower eye pressure.

Atropine sulfate

is a medication that acts as an antidote for certain types of poisoning, particularly those caused by organophosphate insecticides or nerve agents. It works by blocking the effects of acetylcholine, a neurotransmitter that plays a crucial role in various bodily functions.  

CHOLINERGIC AGONIST

1. Direct acting -stimulates the muscarinic and nicotinic receptors

2. Indirect acting

3. Drugs with cholinergic effects on the ANS may have significant effects on neuromuscular transmission

4. Anti-cholinesterase inhibitors block the metabolic effects of the enzyme acetylcholinesterase inactivating acetylcholine.

   • Neostigmine

   • Physostigmine

   • Edrophonium

   • Pyridostigmine

   • Donezepril

CHOLINERGIC CRISIS

muscular weakness, increased salivation, flushing, sweating, abdominal cramps

CHOLINERGIC ANATAGONIST

1. Muscarinic antagonist, anticholinergics, cholinergic

   blocking agents, antispasmodics, parasympatholytics

2. Heart, respiratory tract, GIT, urinary bladder, eyes,

   exocrine glands

3. Dec. GI motility, salivation, dilation of pupils, inc. PR

4. Atropine

Atropine

is a medication that blocks the effects of acetylcholine, a neurotransmitter that plays a crucial role in various bodily functions. It's derived from the deadly nightshade plant.

NEUROTRANSMITTERS

1. Dopamine

2. Serotonin (5-HT)

3. Norepinephrine/ Adrenaline

4. GABA (Gamma-Aminobutyric Acid)

5. Glutamate

6. Histamine

7. Acetylcholine

8. Opiates

DOPAMINE stands for

Drive
psychOsis
Parkinsonism
Attention
Motor
Inhibition of Prolactin
Narcotic
Extrapyramidal

SEROTONIN

also known as 5-hydroxytryptamine (5-HT), is a neurotransmitter that plays a crucial role in regulating various bodily functions, particularly mood, appetite, sleep, and learning. HEAD, FED AND RED

NOREPINEPHRINE

also known as noradrenaline, is a neurotransmitter and hormone that plays a crucial role in the body's "fight-or-flight" response. It's produced by the adrenal glands and certain neurons in the brai

GABA (Gamma-Aminobutyric Acid)

a key neurotransmitter in the central nervous system (CNS). It is primarily inhibitory, meaning it reduces the activity of neurons, helping to regulate neuronal excitability and maintain balance in the brain's electrical activity.

GLUTAMATE

is the most abundant excitatory neurotransmitter in the central nervous system (CNS). It plays a crucial role in brain function, including learning, memory, and neural communication.

HISTAMINE

THE BODY’S ALERT SYSTEM is a chemical compound produced by the body's immune system. It plays a crucial role in various bodily functions, most notably in the body's inflammatory response.

ACETYLCHOLINE

A utonomic Nervous System
C ontraction of muscle
H OTS (Higher-Order Thinking Skills)

OPIODS (ARMED CHINESE)

A nalgesia
R espiratory Depression
M iosis
E uphoria
D rowsiness

C onstipation

PRINCIPLE OF NEUROTRANSMITTERS

1. What comes up, must go down.

2. A neurotransmitter is not easily fooled.

3. With great power comes greater responsibility.

WHAT PSYCHOPHARMA DOES

1. Full Agonist

2. Partial Agonist

3. Neutral Antagonist

4. Inverse Agonist

2 TYPES OF PSYCHOPHARMA

1. Therapeutic Drugs

2. Recreational Drugs

CLASSIFICATION OF PSYCHOPHARMACOLOGIC DRUGS

1. Antidepressant

2. Mood Stabilizers

3. Antipsychotics/Neuroleptics

4. Anxiolytic and Hypnotics

5. CNS Stimulants

ANXIOLYTICS

are medications or agents that help reduce anxiety. They are used to manage conditions like generalized anxiety disorder (GAD), panic disorder, and other anxiety-related conditions. These drugs work by modulating the activity of the central nervous system (CNS) to induce a calming effect.

ANXIOLYTICS

1. Anxiolytics lyse the feeling of anxiety

2. Increases GABA

3. Used in the treatment of anxiety disorders, alcohol withdrawal, hyperexcitability and agitation, and preoperative medication.

4. acts on the limbic system and RAS

5. Benzodiazepines

6. Barbiturates

BENZODIAZEPINES

are a class of psychoactive drugs primarily used for their anxiolytic, sedative, muscle relaxant, anticonvulsant, and hypnotic properties. They work by enhancing the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA-A receptor, leading to increased inhibitory neurotransmission in the central nervous system (CNS).

Barbiturates

are a class of sedative-hypnotic drugs that depress the central nervous system (CNS). They were historically used for sedation, anxiety, seizure control, and anesthesia induction but have largely been replaced by safer alternatives like benzodiazepines due to their high risk of dependency, overdose, and narrow therapeutic index.

BENZODIAZIPINES

1. Decreased toxicity and overdosage

2. Sedating

3. Effective for short-term use

   • Short-acting - panic attacks/status epilepticus

   • Medium acting - anxiety, insomnia, panic ds’

   • Long-acting - panic disorder, alcohol withdrawal

Anxiolytics Across the Lifespan

1. CHILDREN

   • Unpredictable responses seen in children such as aggressiveness, crying, irritability, and fearfulness

2. ADULT

   • Short term use for insomnia

   • Advise not to drive or operate machinery

   • Explore other methods to induce sleep

3. OLDER ADULTS

   • More susceptible to the adverse effects of the drugs

   • Reduced doses

   • Non pharmacological measures should be explored

ANTIDEPRESSANT AGENTS

1. Tricyclic Antidepressants

2. Selective Serotonin Reuptake Inhibitors

3. Monoamine Oxidase Inhibitors

4. Atypical Antidepressants

5. Sedative - Hypnotics

TRICYCLIC ANTIDEPRESSANTS

1. The oldest among the antidepressants used

2. Inhibits presynaptic reuptake of NE and serotonin which leads to an increase of these NT increasing the stimulation of the receptors

3. Relieves the symptoms but has a delayed effect

4. Also indicated for panic disorders, OCD, eating disorders

5. Side Effects: EPS, tardive dyskinesia, neuroleptic malignant syndrome

SELECTIVE SEROTONIN REUPTAKE INHIBITOR

1. Effective for most patients

2. Inhibits the transporter on the presynaptic neurons that take serotonin back up to the cell effectively increasing serotonin

   active and available in the synaptic cleft.

3. Indicated for depression, OCD, panic attacks, bulimia, premenstrual dysphoric disorder, PTSD, social phobia, and social anxiety disorders.

4. Maximum efficacy is not reached within 4-6 weeks

5. Safer for use in children as well as adults because it is less

   sedating, lesser anticholinergic effect and cardiovascular effect.

MONOAMINE OXIDASE INHIBITORS

1. Potential fatal side effects and numerous drug interactions thus the use is infrequent.

2. Blocking the breakdown of the biogenic amines NE, dopamine, and serotonin allow these amines to accumulate in the synaptic cleft and in the neuronal storage vesicles, causing increased stimulation of the postsynaptic receptors.

3. Primarily indicated for depression who cannot tolerate the safer antidepressants.

HYPERTENSIVE CRISIS

1. Fatal adverse effect

2. MAOI + Tyramine Interaction

3. Occipital headache, hypertension, nausea and vomiting, fever, motor agitation, cerebral hemorrhage, death

4. Occurs within 20-30 minutes after ingestion

5. ABC’S

ATYPICAL ANTIDEPRESSANTS

1. Blocks serotonin, NE, dopamine weakly

2. Can be used in client’s with liver and renal diseases

3. Increased incidence of weight gain, sedation, and anticholinergic effects.

4. Bupropion - smoking cessation

5. Selegiline - Parkinson’s

6. Trazodone- adults and pediatric patient aged 6-18

BUPROPION

is an atypical antidepressant with unique properties that make it different from other antidepressants. It is commonly used to treat major depressive disorder (MDD), seasonal affective disorder (SAD), and as a smoking cessation aid.

SELEGILINE

is a medication that acts as a selective monoamine oxidase B (MAO-B) inhibitor. It is commonly used in the treatment of Parkinson’s disease and sometimes in major depressive disorder (MDD). By inhibiting the breakdown of certain neurotransmitters, it helps increase their levels, providing therapeutic benefits.

TRAZODONE

is an atypical antidepressant primarily used for the treatment of major depressive disorder (MDD) and insomnia. It is notable for its sedative properties, which often make it a preferred choice for patients with depression accompanied by sleep disturbances.

ANTIDEPRESSANTS THERAPHY ACROSS THE LIFESPAN

1. CHILDREN- drug affects are unpredictable in children

   • Higher suicidal ideation and behavior

   • TCA (clomipramine, imipramine, nortriptyline, and trimipramine) have established therapeutic doses

2. ADULTS- rule out medical cause of depression

   • use cautiously during pregnancy and lactation

3. OLDER ADULTS- more susceptible to adverse effects

   • Reduced doses; screen for renal and hepatic impairment

SEDATIVE-HYPNOTICS

1. Commonly ordered for sleep disorders.

2. Diminishes physical and mental responses.

3. Ramelton is the only major sedative-hypnotic approved for long term use

4. Barbiturates

5. Benzodiazepines

ANTIMANIC AGENTS

1. Lithium salts

2. Anticonvulsants

LITHIUM SALTS

is a mood stabilizer widely used for bipolar disorder, particularly for managing mania and reducing the risk of mood episode recurrence. It is also used off-label for treatment-resistant depression

ANTICONVULSANTS

also known as antiepileptic drugs (AEDs), are medications primarily used to treat seizure disorders such as epilepsy. Additionally, many anticonvulsants are effective for managing mood disorders, neuropathic pain, and migraine prevention due to their ability to stabilize neuronal activity

ANTIMATIC AGENTS

also known as mood stabilizers, are medications used to treat and manage mania and related mood symptoms in conditions such as bipolar disorder. They help stabilize mood, prevent mood swings, and reduce the severity and frequency of manic and depressive episodes.

ANTIPSYCHOTICS

1. Aka Neuroleptics

2. Essentially dopamine-receptor blockers that acts on the primary pathway of psychosis

3. Typical and atypical antipsychotics

4. Indicated for use in schizophrenia and for manifestation of psychotic disorders

ANTIPSYCHOTICS

are a class of medications used primarily to manage psychotic disorders such as schizophrenia, bipolar disorder, and psychosis associated with other conditions. They may also be used off-label for agitation, severe depression, and certain behavioral disorders.

Thorazine (Chlorpromazine)

is a first-generation antipsychotic (FGA) and is one of the classic typical antipsychotics. It was the first antipsychotic drug developed and remains used for various psychiatric conditions, though it is less commonly prescribed today due to the availability of newer agents with fewer side effects

Chlorpromazine

(brand name Thorazine) is a first-generation antipsychotic (FGA) that belongs to the phenothiazine class of drugs. It was the first antipsychotic medication to be developed and remains in use for various psychiatric and non-psychiatric conditions. Chlorpromazine is often used to treat schizophrenia, acute psychosis, and other mood disorders.

Haldol (Haloperidol)

is a first-generation antipsychotic (FGA) medication in the butyrophenone class. It is one of the most widely prescribed typical antipsychotics, known for its potent dopamine receptor antagonism. It is commonly used to manage schizophrenia, acute psychosis, and other psychiatric disorders.

Clozapine

is an atypical (second-generation) antipsychotic medication that is primarily used for treatment-resistant schizophrenia and for reducing the risk of suicidal behavior in people with schizophrenia. It is considered one of the most effective antipsychotics for patients who do not respond well to other medications, but it also carries a risk of serious side effects, which require careful monitoring.

Olanzapine

is an atypical (second-generation) antipsychotic commonly used to treat schizophrenia, bipolar disorder, and other psychiatric conditions. It is part of the thienobenzodiazepine class and is often chosen for its effectiveness in treating both positive and negative symptoms of schizophrenia, as well as its mood-stabilizing effects.

Risperidone

is an atypical (second-generation) antipsychotic that is primarily used to treat schizophrenia, bipolar disorder, and irritability associated with autism. It is considered one of the more commonly prescribed antipsychotics due to its efficacy in managing both positive and negative symptoms of schizophrenia, as well as its relatively favorable side effect profile compared to first-generation antipsychotics.

Quetiapine

is an atypical (second-generation) antipsychotic commonly used to treat schizophrenia, bipolar disorder, and major depressive disorder (MDD). It is often preferred for its relatively mild side effect profile compared to first-generation antipsychotics and its efficacy in treating both positive and negative symptoms of schizophrenia as well as mood stabilization in bipolar disorder.

Aripiprazole

is an atypical (second-generation) antipsychotic commonly used to treat schizophrenia, bipolar disorder, and major depressive disorder (MDD). It is distinct from other antipsychotic medications due to its partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors, which contributes to its unique pharmacological profile.

Extrapyramidal Symptoms

1. Acute dystonic reactions - spasms of discrete muscle groups such as neck and eye muscles.

2. Akathisia - restless movement, pacing inability to remain still, “inner restlessness.”

3. Parkinsonism - “pseudo parkinsonism”, shuffling gait, mask-like facies, muscle stiffness, cogwheel rigidity, drooling, akinesia. Aka “Thorazine Shuffle”

TARDIVE DYSKINEA

1. Late appearing side effect characterized by involuntary abnormal movements

2. Lip smacking

3. Tongue protrusion

4. Chewing

5. Blinking

6. Grimacing

7. Choreiform movements of the limbs

Tardive Dyskinesia (TD)

is a serious and often irreversible movement disorder caused by the long-term use of antipsychotic medications(particularly first-generation antipsychotics or neuroleptics). It is characterized by involuntary, repetitive movementsthat most commonly affect the face, mouth, and tongue, but can also involve the limbs, torso, and other parts of the body.

NEUROLEPTIC MALIGNANT SYNDROME

1. Serious frequently fatal condition

2. Muscle rigidity, high fever, increased muscle enzyme, leukocytosis

Antipsychotics Across the Lifespan

1. CHILDREN

   • The dose is often higher for children

   • Monitor for adverse effect and developmental progress

2. ADULT

   • Monitor regularly, periodic monitoring is warranted

   • Precaution during pregnancy

3. OLDER ADULTS

   • more susceptible to adverse effects

   • Reduced doses

   • Not to be used to control dementia symptoms

CNS STIMULANTS

1. Clinically used to treat attention deficit disorders, behavioral syndromes, and narcolepsy

2. Redirects and excite the arousal stimuli from RAS by increasing the release of catecholamines from presynaptic neurons leading to increase in stimulation of the postsynaptic neurons.

AMPHETAMINES

1. Stimulate the release of the neurotransmitters NE and Dopa from the brain and SNS and inhibit reuptake of these transmitters.

2. High potential for abuse, tolerance, and dependence.

3. 9-13 hours half-life

4. Methylphenidate (Ritalin)

Methylphenidate (Ritalin)

is a central nervous system stimulant commonly prescribed to treat Attention Deficit Hyperactivity Disorder (ADHD) and Narcolepsy. It works by affecting certain chemicals in the brain and nerves that contribute to hyperactivity and impulse control.

ANOREXIANTS AND ANALEPTICS

1. Hypothalamic and limbic regions of the brain to suppress appetite.

2. Affects brainstem and, spinal cord, and cerebral cortex

3. Stimulates respirations

4. Caffeine and Theophylline

Anorexiants (Appetite Suppressants)

are drugs that reduce appetite and are primarily used for the management of obesity or weight loss. They work by altering the chemicals in the brain that control hunger, leading to reduced food intake. These medications are typically used in conjunction with a healthy diet and exercise

Analeptics (CNS Stimulants)

are a group of central nervous system stimulants that are primarily used to treat respiratory depression or to stimulate the CNS in conditions where there is depressed respiratory drive. They are also used to stimulate the central respiratory centers in the brain and to manage conditions like sleep apnea and preterm infants with respiratory problems.

ALCOHOL

1. CNS depressant but a stimulant initially.

2. Easily absorbed and crosses BBB

3. Orally fixated

4. Intoxication

5. Blackout

6. Overdose

Alcohol Withdrawal

1. Onset 4-12 hours after cessation, peaks on the 2nd day

2. Coarse hand tremors, increased PR and BP, delirium tremens, insomnia, N/V, anxiety

3. Psychopharmacology

   • Benzodiazepines

   • Disulfiram

   • Naltrexone

   • SSRI’s

   • Ondansetron

SEDATIVE, HYPNOTICS, ANXIOLYTICS

1. CNS depressants: barbiturates, non-barbiturates, hypnotics, anxiolytics particularly benzodiazepines

2. Withdrawal: anxiety, diaphoresis, hallucination, seizures

3. Withdrawal and Detox:

   • onset depends on half-life

   • opposite of acute effects

   • detox thru tapering

STIMULANTS (SEDATIVE, HYPNOTICS, ANXIOLYTICS)

1. Excites CNS

2. Indicated for ADHD and obesity

3. Rapid intoxication

4. Withdrawal and Detox

   • Hours to days

   • Marked dysphoria

   • Crashing

   • Not treated pharmacologically

CANNABIS

1. Cannabis sativa

2. Marijuana/ Hashish

3. Used for treatment of glaucoma, N/V in chemotherapy, anorexia, weight loss

4. Acts in 1 min after inhalation, peaks in 20-30 minutes and lasts

   2-3 hours

5. Decreased inhibition, increased appetite, euphoria, distortions of time & perception, impaired judgment

6. Physiologic effect: increased appetite, conjunctival injection, dry mouth, hypotension, tachycardia, delirium

7. Withdrawal: muscle aches, sweating, anxiety, tremors

OPIODS

1. Popular choice as it desensitizes user from both psychological and physiological pain and induces a feeling of euphoria and well being.

2. Potent prescription analgesic such as morphine, meperidine, codeine, methadone, and alike.

3. Often abused by health workers.

HALLUCINOGENS

1. Illusions versus hallucinations

2. Distorts users perception of reality and produce symptoms similar to psychosis

3. Increased BP, RR, PR, dilated pupils, hyperflexia

4. Mescaline, LSD, Designer Drugs, Phencyclidine, Anesthetics.

5. Intoxication: anxiety, depression, paranoia, dangerous behaviours, aggression, flashbacks

INHALANTS

1. Diverse groups of drugs

   • Anaesthetics

   • Nitrates

   • Organic solvent

2. Aliphatic and aromatic hydrocarbons found in gasoline, glue, paint.

3. Causes brain damage, PNS damage, and liver damage

4. Intoxication involves dizziness, nystagmus, lack of coordination,

   slurred speech, tremors, muscle weakness.

ANTISEIZURE DRUGS

1. Aka Anticonvulsants or Antiepileptics

2. Stabilize nerve cell membranes and suppress abnormal electrical. Impulses in the cerebral cortex.

3. Hydantoins

4. Long acting Barbiturates

5. Succinamides

6. Benzodiazepinnes

7. Carbamazepine

8. Valproate

ANTICONVULSANTS

1. Miscellaneous anticonvulsants; mood stabilizing

2. Increases the brains threshold to stimulation and

   prevents it from being bombarded with both external

   and internal stimuli

3. Carbamazepine- CBZ

4. Gabapentin

5. Topiramate

6. Valproic acid

ANTI-PARKINSONS

1. Dopaminergic

2. Dopamine Agonist

3. MAO-B Inhibitors

4. Anticholinergics

5. COMT (catechol-O-methyltransferase) inhibitors

Anti-Parkinson's drugs

are medications used to treat Parkinson's disease, a progressive neurodegenerative disorder that affects movement. The primary symptoms of Parkinson's disease include tremors, rigidity, bradykinesia (slowness of movement), and postural instability. These symptoms are caused by the loss of dopamine-producing neurons in the brain.

ACETYLCHOLINESTERASE/CHOLINESTERASE INHIBITORS

1. Permits more Ach in the neuro receptors.

2. Drugs used for Alzheimer Disease

3. Donepezil (mild.moderate, severe AH)

4. Memantine

5. Galantamine

6. Rivastigmine

ACETYLCHOLINESTERASE INHIBITORS

1. Treatment for Myasthenia Gravis

2. Drugs act to inhibit the action of the enzyme that degrades acetylcholine

3. Neostigmine/ Pyridostigmine

4. Steroids

IMMUNOMODULATORS

1. Treatment for Multiple Sclerosis

2. Disease Modifying Drugs

3. Beta 1b

4. Glatiramer

5. Teriflunomide

6. Steroids