PHARMACOLOGY 1

WEEK 11 / Ma’am Maria Suzette Agluba

DRUGS FOR PSYCHOSIS
PSYCHOSIS ▪ Delusions of thought broadcasting
• Denotes a variety of mental disorders (Nasa isip mo minamarites ka
lagi/Pinaguusapan)
SCHIZOPHRENIA ▪ ” Delusions of persecution” (They

• Clear sensorium but a marked thinking believe na laging may harm).

disturbance ▪ Delusions of reference – “center of

• Malinaw yung senses but pag dating sa brain nag attention” (They believe they are the

iiba kaya nag cacause ng hallucinations center of attention/Nakikinig lang sya

sa radio, then may nag congrats, iniisip
nya sya yon)
Course of Schizophrenia
▪ Thought withdrawal (They believe that
Prodomal phase:
their thoughts can be remove)
o Onset and build up of schizophrenic
▪ Capgras’s syndrome – “double” (They
symptoms (Can be seen aura and next is
believe they have twin or double)
auditory
• Perceptual distortion (hallucinations): Sensory
Active phase:
perceptions not directly attributable to
o Full-blown symptoms: severe disturbances
environmental stimuli (appear real to the
in thinking, deterioration in social
schizophrenic):
relationships, and flat or inappropriate affect
▪ Auditory (hearing)
Residual phase:
▪ Visual (seeing)
o Symptoms no longer prominent
▪ Olfactory (smelling)
o Complete recovery is rare, but
▪ Tactile (feelings)
schizophrenics can lead productive lives.
▪ Gustatory (tasting)
▪ Greatest distress: When voices are
dominant and insulting, and patient lacks
Symptoms of Schizophrenia
communication with the voices
Characteristic symptoms
▪ Coping strategies:
Two or more of the following, each persisting for a
▪ Distraction
significant portion of at least a 1-month period:
▪ Ignoring
Positive symptoms:
▪ Selective listening (to only some of
• Symptoms which are not present in the
what the voices say)
normal individual but are added to the
▪ Setting limits (for example, ‘that
schizophrenic person.
voices can speak to you after 8pm,
• Schizophrenic individual only not normal
but not before’).
individual
Negative symptoms:
• Hallucinations and delusions
• Symptoms involving characteristics, behavior
• Distortions or excesses of normal functioning
or abilities that are present in a normal person
• Delusions: False beliefs firmly and
but missing in the schizophrenic individual.
consistently held despite disconfirming
• Associated with inferior premorbid social
evidence or logic
functioning
▪ Delusions of grandeur (Pinaka sa
• Flat affect (little or no emotion in situations in
pinaka/pusa lang yung present but
which strong reactions are expected)
tigre ang nakikita mo)
▪ alogia (poverty of speech)
▪ Delusions of control (They believe
▪ The failure to respond to questions
other people and animals and thing
or comments
can control them)

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
▪ Malayo ang sagot (tinanong mo
sya kung mahal mo sya, tapos ang
sagot nya sige ingat ka)
▪ Can also take the form of slow or
delayed responses
▪ Avolition
▪ (inability to take action or to
become goal oriented)
▪ Inactivity or early loss of interest in
ongoing activity
▪ May indicate irreversible neuronal
loss in a structurally abnormal brain
• Asociality
▪ Inability to form close personal
relationships
▪ Anhedonia:
▪ Inability to feel pleasure
Disorganized Symptoms
• Disorganized speech (Formal thought
disorder)
• Incoherence
▪ Inability to organize ideas
• Loose associations (derailment)
▪ Rambles, difficulty sticking to one topic
• Odd or peculiar behavior
▪ Silliness, agitation, unusual dress
▪ e.g., wearing several heavy coats in hot
weather
Other symptoms
• Catatonia
• Motor abnormalities
• Repetitive, complex gestures
• Usually of the fingers or hands
• Excitable, wild flailing of limbs
• Catatonic immobility
• Maintain unusual posture for long period of
time e.g., stand on one leg
• Waxy flexibility
• Limbs can be manipulated and posed by
another person
• Inappropriate affect
• Emotional responses inconsistent with
situation
▪ Catatonic
▪ Undifferentiated
▪ Residual
PARANOID SCHIZOPHRENIA
• Characterized by one or more systematized
delusions or auditory hallucinations and the
absence of such symptoms as disorganized
speech and behavior or flat affect
• People wake up in the same delusions every
day, rather than having disorganized
delusions
• Includes mostly positive symptoms.
• Responds more readily to medication than
other forms.
• Most common symptom: Delusions of
persecution
DISORGANIZED SCHIZOPHRENIA
• Formerly hebephrenic schizophrenia:
• disorganized behaviors manifested by
disorganized speech and behavior, and flat or
grossly inappropriate affect
• Have delusions and hallucinations that are
less organized than those of the paranoid
schizophrenic, and have disorganization of
thought, behavior and emotion.
• Speech may become incoherent and the
person may invent new words (neologisms).
CATATONIC SCHIZOPHRENIA
• Includes significant disturbance of motor
activity
• Motoric immobility or stupor(withdrawn
catatonia; little or no motor activity)
• Excessive purposeless motor activity
(excited catatonia)
• Extreme negativism or physical resistance
• Peculiar voluntary movements, including waxy
flexibility
• Echolalia orechopraxia (Inuulit nila yung
nakikita at naririnig nila)
• Behavior may become dangerous/violent

Types of Schizophrenia UNDIFFERENTIATED DISORGANIZED

Five types of schizophrenia: SCHIZOPHRENIA
▪ Paranoid • Undifferentiated: Behavior shows prominent
▪ Disorganized psychotic symptoms not meeting criteria for or

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
catatonic into any other paranoid, • Responsible for causing hallucinations
disorganized, schizophrenia (Doesn’t fit • Serotonin 2 activation in brain can cause
category) hallucination
• Related to LSD and Mescaline and other
RESIDUAL SCHIZOPHRENIA drugs activates serotonin 2 receptor
• At least one previous schizophrenic episode • Excess
but current absence of prominent psychotic
features and continuing evidence of 2 or more 2. Dopamine Hypothesis
symptoms, such as marked social isolation, • Excessive dopamine in mesolimbic system
peculiar behaviors, blunted affect, odd beliefs, and striatal-frontal system
or unusual perceptual experiences • Homovanillic acid (HVA)
▪ Showing symptoms of schizophrenia - metabolite of Dopamine (cerebrospinal fluid,
which remain in between episodes or plasma, and urine)
after medication has been used to treat • High HVA metabolite of dopamine
all treatable symptoms. • Mesolimbic system – psychosis
DOPAMINERGIC TRACTS
Psychotic Disorders Once Considered Mesolimbic-mesocotical Behavior
Schizophrenia pathway
Brief psychotic disorder: Nigrostriatal Tract coordination of voluntary
o Schizophrenic episodes that last at least one movement
day but less than one month
Tuberoinfundibular Inhibits prolactin release
Schizophreniform disorder:
Medullary-periventricular Involved in eating
o Schizophrenic episodes that last at least one
behavior
month but less than six months
Incertohypothalamic Regulate the
o Does not require impairment in social or
anticipatory motivational
occupational functioning
behavior

Other Psychotic Disorder

Delusional disorder:
o Holding non bizarre beliefs (situations that
could occur) lasting at least one month;
except for the delusion the behavior is not
odd
o Common themes: grandiosity, jealousy,
persecution, and somatic complaints 
Shared psychotic disorder:
o A person with a close relationship to an
individual with delusional/psychotic believes 1. Antipsychotic drugs block D2 dopamine receptors
comes to accept those beliefs 2. Drugs that increase dopaminergic activity produce
o Folie a deux (Madness shared by two) or exacerbate schizophrenia
3. Dopamine receptor density is increased in
PATHOPHYSIOLOGY schizophrenia patients (Dopamine receptor)
NEUROTRANSMITTER CHANGES 4. PET shows increased D2 receptor density
➢ Dopamine 5. Successful treatment of schizophrenia changes
➢ Glutamate HVA in CSF of patients
➢ Serotonin
(Pag excess need iblock ang dopamine receptor)
1. Serotonin Hypothesis

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
3. Glutamatergic dysfunction o Temporal cortex - smaller and less active than
PENCYCLIDINE & KETAMINE normal
• Ketamine is a general anesthetic which blocks Subcortical atrophy
NMDA o Enlarged ventricles (Maraming na process na
• NMDA antagonist information)
• Produces “schizoprenia- like” symptoms o Smaller hippocampus (esp. for people with

• Glutamate has many receptor which can bind to negative symptoms)

NMDA, glutamate receptors and AMPA o Thalamus is smaller and less active

Ampakines o Smaller amygdala

- drugs that potentiate currents mediated by AMPA o Ventricles (Dito napupunta yung mga waste

type glutamate receptors information in the brain)

- neuroprotective
SCHIZOPHRENIA: Who is at Risk?

Etiology of Schizophrenia Predisposing factors

Biological: •Pregnancy and birth complications (Damage in brain

▪ Genetic, brain-structure, and biochemical development)

explanations •Genetic background

▪ Biochemical explanation – neurotransmitter Precipitating factors

▪ Schizophrenia – biological disease •Stress

•Substance of Abuse

Physiological Factors of Schizophrenia

• High Neurological Activity Management of Schizophrenia

• PET scans show higher levels of activity ➢ Psychosocial therapy

in the prefrontal cortex and temporal ➢ Institutional approaches

cortex of schizophrenic individuals ➢ Cognitive-behavioral therapy

➢ Family communication and education
• Prefrontal cortex (Dito naiintegrate yung
information and under din neto yung
auditory). Very active ito. Psychosocial therapy

• Differences in cerebral glucose metabolism, • Practical advice, getting in touch with one’s

especially during cognitive tasks feelings, understanding one’s effect on others,

understanding reasons for one’s actions and

Physiological Factors of Schizophrenia (cont’d): feelings, and understanding the impact of past

Problems with brain development and activity on present behavior

Reversed hemispheric dominance • Most important quality of therapist: Friendship

o Suggesting that the left hemisphere did not

develop normally and become dominant
Failure of neural migration Institutional approaches

o The movement of neurons to the gray matter
of the cortex during prenatal development
appears retarded
o The movement of neurons to the gray matter
of the cortex during prenatal development
appears retarded
Cortical atrophy
o Atrophy (Matigas na small size)
o Prefrontal cortex – smaller, less active, and
decreasing in size at a faster rate than normal
(hypofrontality)
• Social learning programs: Appropriate self-
care, conversational skills, role skills
• Undesirable behaviors are decreased through
reinforcement and modeling.
Cognitive-behavioral therapy:
• Work at reducing frequency and severityof
positive and negative symptoms
• Enhance coping skills
• Weaken beliefs regarding power/omnipotence
of auditory hallucinations

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
• Challenge false beliefs
• Social skills training emphasizes
communication skills and assertiveness,
encourages functional independence,
improves family relationships
✓Preoperative Sedatives (Promethazine)
✓Neuroleptanesthesia (Droperidol +Fentanyl + Nitrous
Oxide) –
Droperidol and Fentanyl = Neurolepanalgesia

Family communication and education Uses of Neuroleptics

• Normalize family experience
• Educate family members about schizophrenia
• Identify strengths and competencies ▪
• Develop problem solving and stress
management skills
• Learn to cope with symptoms
• Recognize early signs of relapse
• Create supportive family environment
• Understand/meet needs of all family members
Treatment of Schizophrenia
➢ Antipsychotic medication
➢ Neuroleptics – used interchangeably that
treats schizophrenia
ARIPIPRAZOLE
▪ Is prescribed in some cases of Asperger's
syndrome. (Autistic behavior)
▪ Third Generation of antipsychotic
▪ First Generation are the typical antipsychotics
Mechanism of Action of Neuroleptics
• Typical antipsychotics (1st Gen)
• Block the postsynaptic dopamine (D2)
receptors
• Dopamine blocker
• Atypical antipsychotics (2nd Gen)
• Block serotonin receptors
• Dopamine and serotonin blocker

Neuroleptics TYPICAL ANTI-PSYCHOTICS

• Sometimes referred to as major tranquilizers, • Mainly effective against the positive
because some of them can tranquilize and symptoms of schizophrenia
sedate • Pag blinock means no hallucinations
Typical Anti-psychotics - actions
HISTORY Site of dopamine Actions
RESERPINE AND CHLORPROMAZINE Blockade
• First drugs found to be useful in schizophrenia Mesolimbic system Antipsychotic actions •
• Reserpine – storage inhibitor to monoamine to reduce hallucinations
break by enzyme. Side effect: can cause and agitation
depression. Nigrostriatal pathway Extrapyramidal
effects/Parkinsonian like
Clinical Uses of Antipsychotic symptoms
Psychiatric Indications CTZ Anti-emetic effect
✓Schizophrenia Pituitary Increase Prolactin
✓Schizoaffective Disorders release

✓Bipolar Affective Disorder

Antipsychotic – excess dopamine (needs blockage)
✓Tourette’s Syndrome
Parkinson – low dopamine
✓Senile Dementia of Alzheimer type
Neuropsychiatric Indications
TYPICAL ANTIPSYCHOTICS
✓Antiemetic ( Prochlorperazine, Benzquinamide)
1. Phenothiazine
✓Antihistamines (Phenothiazines) • Aliphatic
• Piperidine
• Piperazine
2. Butyrophenone (haloperidol)

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
3. Thioxanthine Chlorpromazine & Thioridazine 25-30% bioavailability
• Eg. Chlorprothixene and Thiothixene Haloperidol 65% bioavailability
Phenothiazine (Three rings) ABSORPTION and DISTRIBUTION:
Aliphatic • Highly lipid soluble
▪ Chlorpromazine • Highly protein bound (92-99%)
▪ Promazine • Large Vd (> 7 L/Kg)
▪ Trifluoropromazine Available in Slow release preparations (IM
Piperidine Injections)
▪ Thioridazine • Fluphenazine decanoate
▪ Mesoridazine • Haloperidol decanoate
▪ Piperacetazine
Piperazine – more potent, more selective
CHLORPROMAZINE
▪ Fluphenazine
▪ First antipsychotic developed as a surgical
▪ Perphenazine
anesthetic
▪ Acetophenazine
▪ Called as dirty drug due to its capability to block
▪ Trifluorophenarine
other receptors
▪ Prochlorperazine
▪ Receptors blocked:
•Adrenoceptors - Hypotension
Antipsychotic/Neuroleptics •Serotonin
Which is the Most Potent? Piperazine •Histamine 1 –sedation
•Muscarinic - Constipation, dryness
•Dopamine blockade - Parkinsonian syndrome
▪ Metabolic effects
•Decrease gonadotropins
•Decrease pituitary growth hormones
•Increase prolactin
▪ Cholestatic jaundice (rare)

MESORIDAZINE
▪ Major metabolite of Thioridazine (piperidine)
▪ More potent than the parent compound and
accounts for most of the effect.

Next potent is aliphatic. If the patient is diagnosed in

HALOPERIDOL (Haldol©)
schizophrenia, the first drug will be aliphatic. If there
▪ non-selective neuroleptic
is a tolerance in aliphatic, there are some other drugs
▪ EPS is common
that can be used to treat the disease.

Atypical Second Generation Neuroleptics

Uses of Phenothiazine
The mechanism of action of second-generation
▪ Management of psychotic disorders
neuroleptics
▪ Control of manic depression
▪ Blockade of 5HT2A receptors
▪ Relief of acute intermittent porphyria
Receptors Blocked:
▪ Adjunct in the treatment of tetanus
• 5-HT2, 5-HT6 and 5-HT7
Uses of Phenothiazines (cont.)
Others:
• Treatment of severe nausea and vomiting
• alpha-1 adrenergic receptors
• Chlorpromazine - for intractable hiccups
• dopamine receptors in the mesolimbic and
• Promethazine – antipruritic
mesofrontal systems.

Pharmacokinetics of Phenothiazine

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
Inverse Agonist – 5HT2A ▪ Reserve drug for severely schizophrenic patients
• Produces opposite response who are refractory to traditional therapy.
• Used as drug antagonist
o Melperone OLANZAPINE (Zyprexa)
o Zotepine ▪ For certain people with schizophrenia who take
o Risperidone perphenazine first and get no or minimal benefit
o Blonanseine and/or experience intolerable side effects.
o Olanzapine ▪ Zyprexa is not a good option for people who are
o Aripiprazole overweight, have blood sugar abnormalities,
o Quetiapine diabetes, or heart disease.
o Ziprasidone
o sertindole TYPICAL ATYPICAL
o Paliperidone Haloperidol Risperidone
o Iloperidone Chlorpromazine Clozapine
o Asenapine Thiodazine
o Lurasidone Blocks D2 receptors Blocks D2. And 5-
5HT2c HT2 (Risperidone)
▪ Modulates cortical and limbic dopaminergic Blocks D1 and 5-
activity HT2 (clozapine)
Inverse agonists – 5HT2C Treats positive Treats both positive
o Clozapine symptoms only and negative
o Asenapine symptoms
o Olanzapine Causes movement Little or no
Atypical Anti-Psychotics disorders movement disorders
o Dibenzoxazepine – Loxapine
o Dibenzodiazepine – Clozapine Summary of Adverse Effects
o Benzisoxazole – Risperidone ANS
o Thienobenzodiazepine – Olanzapine ▪ Muscarinic receptor blockade :
o Fluorophenylindole – Sertindole •Loss of accommodation
o Quetiapine •difficulty in urination
o Sulpride and sulpiride •Constipation
•toxic- confusional state
RISPERIDONE ▪ Alpha adrenergic blockade :
▪ more selective than the older ‘typical’ neuroleptics •Chlorpromazine - Orthostatic hypotension (the
▪ Exhibits low incidence of EPS and tardive most common cardiovascular effect)
dyskinesia •Mesoridazine -Failure to ejaculate
▪ Included in the first line agents •Impotence
▪ CNS - Dopamine receptor blockade
PALIPERIDONE (9-hydroxyrisperidone) ▪ EPS
▪ Active metabolite of risperidone ▪ Prolactin elevation
•Amenorrhea, galactorrhea, infertility

CLOZAPINE ▪ Dopamine receptor hypersensitivity:

▪ antipsychotic effects : 5-HT 2A/2C and D2 o Tardive dyskinesia (involuntary movements

receptor antagonism. of the face or limbs)

▪ more potent antagonism at the D4 receptor than o Increase dose suppresses of the condition

the D2 receptor. • Tardive akathisia (Extreme restlessness) – Long

▪ Lowest likelihood in producing EPS and tardive term treatment  Decrease dopamine receptor

dyskinesia sensitivity  Need of increase the dose

Peñafiel, D. & Reynon, R. (2022)

DRUGS USED FOR PSYCHOSIS
o choreoathethoid movements
o Tongue protrusion/twisting,lip puckering
o Risk: elderly, long-term
o female,
o Onset: years after tx
o Tx: lower dose, change meds
• Akathisia
o Subjective feeling of muscular discomfort
o Agitated, pace relentlessly, alternately sit and
stand
o Risk: recent increase/onset of meds
o Onset: 1st month of therapy
o Tx: beta-blockers (propranolol), BZDs
(lorazepam), clonidine
• Endocrine – Hyperprolactinemia
• Serotonin 5-HT2 blockade
o Fluphenazine (Prolixin) - Available in
decanoate (long-acting) form
o Perphenazine (Trilafon)
o Prochlorperazine (Compazine)
o Thioridazine (Mellaril)
o Trifluoperazine (Stelazine)
o Mesoridazine
o Promazine
o Triflupromazine (Vesprin)
o Levomepromazine (Nozinan)
o Promethazine (Phenergan)
Butyrophenones
o Haloperidol (Haldol)
Thioxanthenes
o Chlorprothixene
o Flupenthixol (Depixol and Fluanxol)

⚫ Orthostatic hypotension o Thiothixene (Navane)

o Zuclopenthixol (Clopixol & Acuphase)
⚫ Sedation
Third generation antipsychotics
⚫ Weight gain
o Aripiprazole (Abilify)
Other Adverse Effects
o Seizures – Clz, Chlorpromazine (Many side
effects due to many receptors blocked)
o Agranulocytosis – Clozapine
o Cardiotoxicity – Thioridazine
o Prolong QT interval – Ziprasidone, Sertindole
o Cornea/Lens deposit – Chlorpromazine
o Retinal deposits – Thioridazine
o Neuroleptic Malignant Syndrome

Neuroleptic Malignant Syndrom (NMS)

▪ idiosyncratic, life-threatening
▪ Motor: Muscular rigidity, dystonia, agitation
▪ Autonomic: hyperpyrexia, hypertension
▪ Risk: high-dose, rapid dose escalation,
▪ IM injection, prior history
▪ Onset: usually within first few weeks
▪ Long term used of antipsychotic drugs
▪ Tx: discontinue meds, supportive, dantrolene,
bromocriptine
▪ Dantrolene – manage muscle rigidity (Relaxant)
▪ Bromocriptine – dopamine agonist
▪ Malignant hyperthermia – Combination of
succinylcholine and hyalophane – Drugs:
Dantrolene

First generation antipsychotics

Phenothiazines
o Chlorpromazine (Thorazine)

Peñafiel, D. & Reynon, R. (2022)

 QUIZZES

QUIZ 6: AUTONOMIC AND PARASYMPATHETIC 14. Reserpine, an alkaloid from Rauwolfia, can lower blood
NERVOUS SYSTEM pressure and depress the CNS. What enzyme or part of the
1. A reversible cholinesterase inhibitor indicated for the biosynthetic pathway is inhibited by Reserpine to bring
treatment of Alzheimer’s disease. about these effects?
Ans: Donepizil Ans: Storage of catecholamines in the presynaptic
2. The cholinesterase inhibitor that is used in the diagnosis of a vesicles
condition in which there is an antibody that disrupts Nm 15. The enzyme that is inhibited by nerve gases such as sarin,
receptor. soman and tabun is:
Ans: Edrophonium Ans: Acetylcholinesterase
3. This drug is used to prevent or reduce the occurrence of 16. A partial agonist of muscarinic receptor that can be used for
nausea and vomiting associated with motion sickness. smoking cessation.
Ans: Scopolamine Ans: Nicotine
4. System activated during stressful situations such as anxiety 17. Which of the following nerve gases contain cyanide in its
and fear. molecule?
Ans: Sympathetic Nervous System Ans: Tabun
5. Which of the following anitmuscarinic drugs is used by 18. Calcium ion stimulates the entry of tyrosine in the
inhalation in the treatment of bronchial asthma? presynaptic nerve terminal. Tyrosine is the precursor in the
Ans: Ipratropium biosynthesis of catecholamines.
6. In comparison to other antimuscarinic agents, Scopolamine is Ans: First statement is FALSE. Second statement is
expected to exert significant CNS effects due to: TRUE.
Ans: Its being a tertiary amine 19. Which of the following is an example of an Ionotropic
7. Which of the following can be used in the management of early receptor (Type 1)?
onset of dementia? Ans: Nicotinic muscular (Nm)
I. Cognex 20. The first orally active sympathomimetic drug.
II. Aricept Ans: Ephedrine
III. Mytelase 21. Inhibits the storage of dopamine and other catecholamines.
IV. Tensilon Ans: Reserpine
Ans: I & II 22. Which of the following drugs are alpha-2 receptor agonists
8. A neuromuscular blocking agent that can cause muscarinic and are used in the management of hypertension?
response such as bradycardia, and increased glandular I. Tolazoline
secretion. Some of its side effects also include neuroleptic III. Clonidine
malignant syndrome, rhabdomyolysis and hyperkalemia. II. Guanadrel
Ans: Succinylcholine IV. Methyldopa
9. It is a drug that can reactivate cholinesterase enzyme by Ans: III and IV
means of removal of phosphoryl group that is bound to the 23. All of the following are expected organ effects of sympathetic
ester group. stimulation EXCEPT:
Ans: Pralidoxime I. Tachycardia III. Bronchodilation II. Miosis TV. Sweating
10. A ganglionic blocker that is considered as among the last line Ans: II only
drugs for hypertensive emergencies: 24. SAR of sympathomimetic agents:
Ans: Trimethaphan 1. Substitution in the terminal amino group increases
11. In the adrenal medulla, noradrenaline is converted to activity in the alpha receptor
adrenaline by the action of which enzyme? 2. Substitution in alpha carbon makes the drug resistant to
Ans: Phenylethylamine N-methyl transferase monoamine oxidase.
12. Mytelase is an example of: 3. Methyl substituent is present in the terminal amino group
Ans: Acetylcholinesterase inhibitor of Isoproterenol.
13. Oxybutinin, Dicyclomine, and Glycopyrrolate are clinically Ans: One of the choices
useful for which of the following conditions? 25. The relaxation of bronchioles, increase uptake of potassium
Ans: Gastrointestinal hypermotility and urinary in the cells, and relaxation of the uterine smooth muscles
incontinence

Peñafiel, D. & Reynon, R. (2022)

 QUIZZES

are associated with: 12. Which of the following drugs are alpha-2 receptor
Ans: Activation of Beta 2 Receptors agonists and are used in the management of
QUIZ 7: ADRENERGIC AGONIST hypertension?
1. SAR of sympathomimetic agents: I. Tolazoline III. Clonidine
a. Substitution in the terminal amino group II. Guanadrel IV. Methyldopa
increases activity in the alpha receptor. ANS: III and IV
b. Substitution in alpha carbon makes the drug 13. All the following statements are true concerning the use
resistant to monoamine oxidase. of dopamine EXCEPT:
c. Methyl substituent is present in the terminal • At small doses, dopamine stimulates the
amino group of Isoproterenol. dopamine-1 receptor which results in increased
ANS: One of the choices is correct renal blood flow and increase diuresis.
2. Indications/uses of epinephrine: • Dopamine is useful in shock conditions
I. Local vasoconstrictor associated with decreased urine output.
II. Asthma • At moderate doses, dopamine can stimulate the
III. Advanced cardiac life support alpha-1 receptor thus producing an inotropic
IV. Cardiogenic shock effect.
ANS: NOT I, III,AND IV • None of these
3. In terms of mechanism of action, which of the following ANS: At moderate doses, dopamine can
closely resembles the action of Catapres®? stimulate the alpha-1 receptor thus producing an
ANS: methyldopa inotropic effect.
4. This drug exerts its antihypertensive effects by producing 14. Dipivefrin is used for:
a false neurotransmitter that preferentially binds to central ANS: Glaucoma
presynaptic alpha-2 receptors, thus producing a negative 15. True about epinephrine:
feedback effect.
I. Metabolized by COMT and MAO
ANS: methyldopa
5. Attention deficit hyperactivity disorder can be treated by II. Also known as adrenaline
which of the following drugs?
III. Contain dihydroxy benzene group
ANS: methylphenidate
6. A patient complains of weakness after several doses of ANS: I,II, AND III
Salbutamol nebulization. This condition can be attributed
to the? 16. This enzyme converts epinephrine into norepinephrine in

ANS: hypokalemia the adrenal medulla?

7. Which of the following is an expected response to alpha- ANS: Phenylethanolamine N-methyl transferase

1 adrenoreceptor stimulation? 17. Which of the following primarily stimulates beta-1

ANS: intestinal sphincter contraction receptors?

8. A beta-2 selective agonist: ANS: Dobutamine

ANS: isoxsuprine 18. Which of the following is true regarding Methyldopa?

9. True of alpha-1 selective agonists EXCEPT: I. It is used in the management of pregnancy-

induced hypertension
• They are used as nasal decongestants
II. It causes dose-dependent hepatotoxicity
• They raise BP during hypotensive states
III. It should not be given at doses of more than 2
• They can be given for > 5 days orally
grams per day
• None of these
IV. It causes false (+) Coomb’s test
ANS: They can be given for > 5 days orally
ANS: I, II, III, IV
10. The immediate precursor in the biosynthesis of
19. Sympathomimetic agents:
norepinephrine:
• Parent molecule is phenylethylamine
ANS: Dopamine
• These can cause withdrawal symptoms
11. The first orally active sympathomimetic drug.
• Inotropic agents
ANS: ephedrine
ANS: TWO ARE CORRECT

Peñafiel, D. & Reynon, R. (2022)

 QUIZZES

20. In the biosynthesis of Norepinephrine, which is 30. An excessive level of 3-Methoxy -4-hydroxymandelic acid
considered the rate-limiting step? is indicative of what disease?
ANS: Pheochromocytoma
ANS: Conversion of tyrosine to DOPA
21. The final product of norepinephrine and epinephrine P.S. may mga naulit na questions since iba ibang source
nanggaling ang correct answers.
metabolism.
ANS: Vanillylmandelic acid
22. The pivalic ester derivative of epinephrine:
ANS: Dipivefrin
23. TRUE regarding epinephrine EXCEPT:
• It can be given orally to provide a systemic
effect.
• It stimulates alpha-receptors at high doses
• It is the first-line drug in the management of
electromechanical dissociation.
• It is used in anaphylactic shock since its
physiologic effects are opposite to that of
histamine.

ANS: It can be given orally to provide a systemic

effect.

24. The beta-3 receptor is associated with one of the

following?
ANS: LIPOLYSIS
25. All of the following are expected organ effects of
sympathetic stimulation EXCEPT:

I. Tachycardia III. Bronchodilation

II. Miosis IV. Sweating

ANS: II ONLY

26. Which of the following drugs inhibit the diffusion of

norepinephrine in the synaptic cleft?
ANS: GUANETHIDINE
27. TRUE regarding Clonidine:
• It can cause a hypertensive crisis if abruptly
withdrawn
• It acts on both presynaptic and postsynaptic
alpha-2 receptors
• Its side effect includes sedation due to its central
effect
• All of the choices
ANS: ALL
28. Alpha-1 adrenoreceptor is an example of:
ANS: G-protein linked receptor

29. The relaxation of bronchioles, increase uptake of

potassium in the cells, and relaxation of the uterine
smooth muscles are associated with:
ANS: Activation of beta-2 receptors

Peñafiel, D. & Reynon, R. (2022)