DrugList1 PAULA

1st
Colloquium Paula Swiontek

Drug Pharmacological Mechanism of action (B) Indications (C)
group (A)

AUTONOMIC NERVOUS
SYSTEM

PILOCARPINE • M-‐cholinomimetic • Stimulation muscarinic receptors • Xerostomia (Sjögrens • Exocrine glands are:
(direct acting) (M1, M2, M3): syndrome) -‐ Sweat, Salivary, Lacrimal,
• Parasympathomimetic -‐ Increased secretion of • Glaucoma à Gastric, Pancreatic,
exocrine glands decreases IOP Intestinal. Mucous of cells
-‐ Contraction iris sphincter + • Decreased tone/lack of resp. tract
ciliary muscle (topically in eye) of tone of GI tract +
à = all PS effects urinary bladder

NICOTINE • N-‐cholinomimetic • Agonist at nicotinic – cholinergic • Smoking therapy • * Neurotransmitters are:
(direct acting) receptors in autonomic ganglia, (quitting) à relief of -‐ Acetylcholine
adrenal medulla, neuromuscular nicotine withdrawal -‐ Beta-‐endorphin
junction, brain à stimulates symptoms -‐ Dopamine
neurons à release of * -‐ Norepinephrine
neurotransmitters à mediate -‐ Serotonin
pleasure, arousal, mood, appetite
• High Conc. à Cardiovascular
effects
-‐ Peripheral vasoconstriction
-‐ Increased BP -‐ tachycardia
• Low conc. à stimulation
chemoreceptors pulmonary +
coronary circuit à reflex
bradycardia + hypotension

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1st Colloquium Paula Swiontek
NEOSTIGMINE • Parasympathomimetic • Blocks cholinesterases (AChE) à • Treatment of • Does not cross blood-‐brain
reversible normally destroys ACh à delay of myasthenia gravis (= barrier à can not be used in
cholinesterase removal of ACh à stays in muscle weakness) alzheimers
inhibitor (synthetic) synaptic cleft à prolonged effect • Reverse effects of
• Indirect acting • Indirectly stimulates nicotinic (N) muscle relaxants (e.g.
and muscarinic (M) receptors à Gallamine &
involved in muscle contraction Tubocurarine)

ATROPINE • M-‐cholinoblocking • Binds & inhibits muscarinic • Mandatory antidote • Toxicity à increased IOP in
drug acetylcholine receptors (M1, M2, for severe closed – angle glaucoma
• Anticholinergic M3, M4, M5) à wide range cholinesterase
(cholinonegative anticholinergic effects inhibitor poisoning
drugs) • Parasympathetic NS à inhibition • Retinal examination
• Non-‐selective salivary & mucous glands • Prevention of
• Long acting (up to 5 • Cardiac à non-‐selective synechiae after
days) muscarinic acetylcholinergic surgery
antagonist (increases HR) • Sinus bradycardia
• Decreased bronchial secretion • Asthma
• Eye à mydriasis by blocking
contraction of circular pupillary
sphincter (normally stimulated by
ACh release) à dilation of pupil

SCOPOLAMINE • Peripheral • Blocks action of ACh on • Pain treatment of • E.g. buscopane
antimuscarinic, autonomic effectors innervated by abdominal, menstrual
anticholinergic agent post-‐ganglionic cholinergic nerves cramps or other
• Non-‐selective & smooth muscles that lack spasmolytic action in
• M-‐cholino antagonist cholinergic innervation GIT
• Minimal activity on actions of ACh • Gall bladder spasms
in nicotinic receptors
• Not centrally active

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EPINEPHRINE • Non-‐selective, • Acts on: • cardiopulmonary • Overdose à extremely
adrenopositive agent -‐ ⍺1 à vasoconstriction resuscitation (CPR) elevated arterial pressure,
-‐ ⍺2 à vasoconstriction • acute anaphylaxis pulmonary edema,
-‐ β1 à positive ionotropic, • angioedema myocardial
chronotropic, dromotropic, ischemia/infarction,
increases BP cardiomyopathy
-‐ β2 à vasodilation, bronchial
smooth muscle relaxation
• Low doses à dilate BVs (β2),
longer action (increases BP in
beginning then decreases)
• High doses à
-‐ constricts BVs
-‐ increases BP (⍺1)
-‐ dilates BVs in heart, brain,
muscle
-‐ constricts BVs of skin, mucosal,
inner organs
-‐ increased O2 demand in
myocardium
-‐ dilates bronchioles, pupils
-‐ increases glycogenolysis,
adiopolysis

NOREPINEPHRINE • Non-‐selective • Acts on: • Acute hypotension • Side effect: Bradycardia à
adrenopositive a gent -‐ ⍺1 à vasoconstriction • Cardiac arrest due to reflector n. vagus tone
-‐ ⍺2 à vasoconstriction increase (because of the
-‐ β1 à positive inotropic, increased BP) – can be
chronotropic, dromotropic, reversed with atropine
increases BP
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• Weaker action than epinephrine
on internal organ smooth muscle,
metabolism & CNS

LEVONORDEFRIN • Selective • Binds to ⍺ 2-‐adrenergic receptors • Topical nasal • Usually pre-‐mixed solution
(Corbadrine) adrenopositive agent in the nasal mucosa à decongestant with (mepivacain)
(⍺2) vasoconstriction • Vasoconstrictor • Similar to epinephrine but
(dentistry) weaker
FELYPRESSIN • Vasopressin agonist • Binds to vasopressin receptor V1a • Vasoconstrictior in • Contraindications:
à contraction of smooth muscle local anesthetic -‐ Pregnancy due to uterus
in vascular bed injections (dentistry) stimulation
• Ingredient of -‐ Angina pectoralis
preparations that (arrhythmia risk due to
have been used for vasoconstrictor property)
treatment of pain &
inflammation of
mouth

ANALGESIC AGENTS &
NSAIDs
MORPHINI • Narcotic analgesic • Pure opioid receptor agonist; • Severe pain • Contraindications:
HYDROCHLORIDUM agent selective to mu receptors (also • Analgesia during labor -‐ Hypersensitivity to
(Morphium) • Opioid receptor binds to kappa & delta) • Acute pulmonary morphine sulfate
agonist • Primary actions in brain through edema -‐ Acute/severe bronchial
transitory stimulation prior to • Chronic severe pain asthma in unmonitored
depression • cancer pain setting or w/o
• CNS à activates analgesic resuscitative equipment
receptors in CNS à reduction in -‐ Known/suspected
transmission of pain signals to paralytic ileus
brain + respiratory depression by
decreasing brain stem respiratory
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center response to CO2 tension +
electrical stimulation
• Decreased gastric, biliary,
pancreatic secretion
• Peripheral vasodilation
• Opioid – induced hypotension due
to histamine release

FENTANYL • Synthetic opioid • Acts primarily on mu receptors • Pain (acute e.g. during • 100-‐150x stronger than
analgesic agent (also kappa + delta) in CNS à surgery) morphine
• Phenylpiperidine analgesia, mood alterations, • Malignant cancer pain • faster onset, shorter duration
derivate euphoria, dysphoria, drowsiness • Anesthesia (combined • significantly depresses
• Decreases respiratory system + with droperidol) à respiratory center
cough reflex neuroleptanalgesia • causes rigidity of muscles
• Pupil constriction • Tachypnea
• Stimulating chemoreceptor trigger • Delirium (post OP)
zone à nausea + committing (esp. • Conscious sedation
in ambulatory or postural syncope • Very severe, acute
patients) pain
• Increased tone, decreased
peristalsis of GIT
• Increased biliary tract pressure
• Increased urinary smooth muscle
tone

TRAMADOL • centrally a cting • works through binding of parent • pain (moderate to • side effects:
• synthetic opioid drug and O-‐desmetyhl-‐tramadol severe) -‐ nausea, constipation,
analgesic agent metabolite to mu-‐receptors (µ-‐ itchiness
• weak opioid opioid receptors) à = better -‐ serotonin-‐syndrome à
metabolite à higher affinity to µ mental changes,
• inhibits re-‐uptake of NA and 5-‐HT hypertension
(neurotransmitter involved in
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descending inhibitory pain
pathway responsible for pain
relief)

ACIDUM • salicylate • Irreversibly acetylates + • Headache • Side effects: à generally
ACETYLSALICYLICUM • antiaggregant inactivates COX-‐1 (low dose) in • Transient mild + infrequent
(aspirin) • NSAID platelets à inhibits thromboxane mucoskeletal pain -‐ High incident of GIT
• Non-‐selective A2 (vasoconstrictor + thrombocyte • Dysmenorrhea & irritation with
aggregant) & prostacyclin pyrexia asymptomatic blood loss,
(vasodilator + antiaggregant) • Decreased mortality increased bleeding time,
formation à antithrombic effect after heart attack bronchospasm, skin
• Platelet COX à more sensitive to • reactions, reye’s
aspirin than endothelium COX à syndrome (not given to
anti-‐aggregation effect at lower kids below 16)
doses than prostacyclin inhibition • Long-‐term low doses (50-‐150
mg/day) à prevention of
heart attack, stroke blood
clot formation à anti-‐
platelet
• High doses (>500mg) à anti-‐
inflammatory, analgesic,
antipyretic activity à NSAID

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PARACETAMOL • Non-‐opioid analgesic • Centrally acting analgesic + • Reduction of fever • Similar efficacy to aspirin but
(Acetaminophen) • Aniline-‐derivative antipyretic with/without minimal • Mild-‐moderate pain no anti-‐inflammatory activity
• Centrally active anti-‐inflammatory properties à limited by peroxides
• Pain reduction mechanism may be present in inflammation
due to inhibition of central (leukocytes) à inhibition
prostaglandin synthesis (central paracetamol
COX2, COX3) + elevation pain • Drug interaction: Para +
threshold Phenytoin
• Decreases fever by inhibiting • Can cause liver damage
formation + release of (main side)
prostaglandins in CNS and by • N-‐acetyl cysteine in case of
inhibition of endogenous pyrogens overdose
at hypothalamic thermoregulatory
center

DICLOFENAC • NSAID • Inhibition of (COX1) & COX2 à • Inflammatory • Side effects:
• Phenylactic a cid inhibition o f p rostaglandin + diseases -‐ GIT ulceration + bleeding,
derivate thromboxane synthesis à anti-‐ (osteoarthritis, increased heart attack
inflammatory, analgesic, anti-‐ rheumatoid arthritis, risk, liver damage
pyretic ankylosing
spondylitis, pain)

IBUPROFEN • NSAID • Inhibition of COX1 & COX2 à • Pain, pericarditis, • GIT ulceration + bleeding,
• Propionic a cid inhibition o f p rostaglandin + inflammatory disease, hypertension, increased
derivate thromboxane synthesis à anti-‐ fever, dysmenorrhea heart attack risk, liver
• Non-‐selective inflammatory, analgesic, anti-‐ damage
pyretic • combination with alcohol à
increased risk stomach
bleeding

KETOROLAC • NSAID • Inhibits COX1 & COX2 à • Severe acute pain • Side effects:
• Acetic acid derivative decreased prostaglandin levels in
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1st Colloquium

Paula Swiontek
• Non-‐selective COX • Total duration of tissues à decreased
-‐ Drowsiness, dyspepsia,
inhibitor therapy <5 days (high postoperative pain and inhibiting
GIT pain, nausea
GIT ulcerations + • Contraindicated before
surgically induced miosis
bleeding) surgery à intense
antiplatelet effect à may
result in increased intra OP
bleeding

METAMIZOLE • NSAID • Inhibition of central COX3 & • Analgesic, antipyretic,
(Novalgin) • Pyrazolone derivate activation of opioidergic + spasmolytic effect
cannabinoid system • Therapy of spastic
• Blocks both PG – dependent and conditions (esp.
PG-‐independent pathways of fever digestive tract) and
induced by lipopolysaccharide fever refractory to
• Spasmolytic effect à inhibited other treatment
release of intracellular Ca2+ as a
result of reduced synthesis of
inositol phosphate
LORNOXICAM • NSAID • Inhibits COX2 to greater extent • Inflammatory • Less side effects than non-‐
• COX2 inhibitor than COX1 à inhibition of PG diseases: selective COX inhibitors
(selective) synthesis à anti-‐inflammatory, osteoarthritis, • COX inhibition selectively à
• Oxicam derivative analgesic, antipyretic rheumatoid arthritis, dose dependent; diminished
juvenile arthritis at higher dosages

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ETORICOXIB • NSAID • Selective reversible inhibition of • Acute pain, • Potential serious
• Selective COX2 COX2 à inhibition of PG synthesis dysmenorrhea, cardiovascular &
inhibitor à a nti-‐inflammatory, a nalgesic, osteoarthritis, gastrointestinal side effects
• Pyrazolone derivative, antipyretic rheumatoid & • No effect on platelets at
coxib juvenile arthritis, usual therapeutic doses
ankylosing • May reduce risk of colon
spondylitis, colorectal cancer
polyps
NIMESULIDE • NSAID • Weakly inhibits COX2 à • Acute pain, • Hepatotoxic!

• Sulfonanilide class decreased PG synthesis à anti-‐ dysmenorrhea, • No antidote available
inflammatory, analgesic, osteoarthritis,
antipyretic rheumatoid &
• Decreases histamine release from juvenile arthritis,
mast cells & inhibits production of ankylosing
platelet – activating factor by spondylitis, colorectal
human basophils polyps

ZOLMITRIPAN • Selective serotonin • Agonist for serotonin (5-‐HT 1B+1D • Acute treatment of • No significant activity at 5-‐HT
receptor antagonist subtype receptors) in cranial migraine with or 2,3,4 receptor subtypes,
• Anti-‐migraine agent arteries & sensory nerves of without aura in adults adrenergic, dopaminergic,
trigeminal system à constriction histamine, muscarinic
of cerebral blood vessels (due to receptors
5-‐HT 1B+1D) à reduces pulsation
which may be responsible for pain
of vascular headache à relief

CODEINE • Natural opium • Binds to mu-‐receptor (opiate • Combination • Effective oral dose range à
alkaloid receptor agonist) anagesics! 30-‐90mg
• Weak analgesic • Exact mechanism of analgesic • Pain (mild-‐moderate) -‐ 30 mg = minimal
effect unknown; may come from • cough medicine analgesia
its conversion to morphine • diarrhea
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• Antitussive effect via direct -‐ 60 mg = little more
depression of medullary cough analgesia with more
reflex nausea + sedation
-‐ 90 mg = intolerable side
effects
• available in combination with
aspirin/paracetamol
(600/650 mg + 60 mg) à
dental pain relief
BENZYDAMINE • locally acting NSAID • inhibition of COX1 & COX2 à • Gingivitis, pharyngitis,
with local anesthetic inhibits PG synthesis mucosal ulceration &
& analgesic properties • inhibits production of pro-‐ inflammation,
inflammatory cytokines (no tonsillitis
ulcerative action) à anti-‐
inflammatory, analgesic, local
anesthetic effect

ANTICONVULSANTS

CARBAMAZEPINE • Anti-‐epileptic agent • Blocks Na+ channels à inhibits • Epilepsy (both partial • Dose-‐related side effect
(anticonvulsant) high frequency repetitive firing in & generalized tonic-‐ -‐ Diplopia, ataxia,
• Specific analgesic for neurons clonic seizures) • Not sedative in therapeutic
trigeminal neuralgia • Acts pre-‐synaptically à decreased • Bipolar depression dose
• Co-‐analgesic synaptic transmission • trigeminal neuralgia • Controlling mania in bipolar
patients

OXCARBAZEPINE • Anticonvulsant • Activity based on 10-‐ • Epilepsy (both partial • Less potent than
• Co-‐analgesic monohydroxy metabolite (MHD) & generalized tonic-‐ carbamezepine
à block of voltage Na+ channels clonic seizures)
à stabilization of hyperexcited • bipolar depression
• trigeminal neuralgia
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neuron membranes à inhibition
of repetitive neuronal discharges

PHENYTOIN • Anticonvulsant • Blocks Na+ channels (enhances • Epilepsy (both partial • Side effects:
• Co-‐analgesic Na+ efflux from neurons of motor & generalized tonic-‐ -‐ Gingival hyperplasia
cortex) & inhibits generation of clonic seizures) -‐ Osteopenia/Osteomalacia
rapidly repetitive Aps • trigeminal neuralgia (vitamin D deficiency) à
• Dose-‐dependent: inhibition of treatment à Vitamin D +
Ca2+ transport by intestinal cells Calcitriol
à vitamin D deficiency
VALPROIC ACID • Carboxylic acid • Blocks sustained high-‐frequency • Absence (petit mal) // • well absorbed, highly bound
derivative firing of neurons à inhibits Na+ complex partial // to plasma proteins
• Anti-‐epileptic influx into cell by voltage Na+ generalized // simple • 4-‐aminobutyric acid (GABA) +
(anticonvulsant) channels à increased polarization partial seizures 2-‐oxoglutarate succinate à
• Anti-‐manic of cell & decreased excitability • Status epilepticus semialdehyde + L-‐glutamate
• Anti-‐migraine • Suppresses synaptic response • Bipolar disorder
• Co-‐analgesic mediated by NMDA receptors • Migraine
(blocks them) • schizophrenia
• Inhibits 4-‐aminobutyrate
transaminase à increased GABA
level in brain à MIGRAINE

TOPIRAMATE • anticonvulsant • blocks repetitive firing of spinal • Epilepsy (both partial
(substituted cord neurons (as phenytoin & & generalized tonic-‐
monosaccharide) carbamazepine) clonic seizures)
• blocks voltage Na+ & Ca2+ • Lennox-‐Gastaut
channels (L-‐type) syndrome
• antagonism of AMPA/kainite • infantile spasms
subtype of glutamate receptor • absence seizures
• potentiates inhibitory effect of
GABA at different sites than
benzodiazepine/barbiturate
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• multiple effects due to primary
action on kinases altering
phosphorylation of voltage &
ligand ion channels

LEVETIRACETAM • Anticonvulsant • Binds selectively to synaptic • Adjunctive treatment
(piracetam a nalog) vesicular protein SV2A (function partial seizures
unknown) à modifies synaptic (adults)
release of glutamate and GABA • Primary generalized
through action on vesicular tonic-‐clonic seizures
function (children)
• Myoclonic seizures
(juvenile
myoclonicepilepsy)
PREGABALIN • Anti-‐epileptic • Binds to ⍺ 2δ-‐ subunit of voltage • Seizure disorders • Well absorbed
(anticonvulsant) Ca2+ within CNS & modulates (partial in adults) • Not bound to plasma
• GABA – analogue with Ca2+ influx at nerve terminals à • Neuropathic pain proteins
anti-‐seizure + inhibits excitatory (post herpetic
analgesic properties neurotransmitter release neuralgia)
• Co-‐analgesic (Glutamate, NA, 5-‐HT, D, • Fibromyalgia
Calcitonin gene – related peptide) • Trigeminal neuralgia
• Modifies synaptic / non-‐synaptic
release of GABA à increased
GABA concentration in brain à
anti-‐nociceptive & anti-‐convulsant

GABAPENTIN • Antiepileptic • Gabapentin & its metabolites à • Seizure disorders • Structurally related to GABA
(Anticonvulsant) do NOT bind to GABA A & GABA B • neuropathic pain • Poor bioavailability
• Amino acid – receptors • vasomator symptoms • Side effects:
• GABA – analogue • Binds to voltage pre-‐synaptic Ca2+ • trigeminal neuralgia -‐ Somnolence
• Co-‐analgesic channels (inhibits ⍺2δ -‐1 subunit) -‐ Dizziness/ataxia
à decreased release of excitatory -‐ Dry mouth
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neurotransmitters (participate in -‐ Peripheral edema
epileptogenesis & nociception) -‐ Blurred vision

LAMOTRIGINE • Antiepileptic • Inhibits voltage Na+ channels à • Epilepsy (partial – • Well absorbed orally
(anticonvulsant) stabilizes neuronal membranes à onset seizures &
• Phenyltriazine suppresses sustained rapid firing generalized seizures)
derivative of neurons • Bipolar disorder
• Acts pre-‐synaptically on voltage
Ca2+ channels (block N-‐type
channel) à Decreased synaptic
release of glutamate

ANTIPARKINSONIAN
AGENTS

LEVODOPA • Anti-‐parkinsonian • Levodopa à levorotary isomer of • Parkinson syndrome
agent dihydroxy-‐phenylalanine &
• Anti-‐muscarinic metabolic precursor of dopamine
• Converted to dopamine after
crossing blood-‐brain-‐barrier à
restores CNS dopamine levels
(usually given with carbidopa or
benserazide à prevent conversion
to dopamine in periphery)
• Most levodopa are decarboxylated
to dopamine before reaching brain
(stratum, palladium, substantia
nigra)

TRIHEXYPHENIDYL • Anti-‐muscarinic (M1 • Direct inhibitory effect on • Parkinson syndrome
antagonist) parasympathetic NS à block of (all forms)
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• Anti-‐parkinsonian efferent impulses; central • Drug-‐induced
• Anti-‐cholinergic inhibition of cerebral motor extrapyramidal
centers symptoms (from
• Relaxing effect on smooth antipsychotic agents)
musculature à directly on muscle
itself & indirectly through
parasympathetic NS
• Positive effect on dopamine
receptors

ANESTHETIC AGENTS

NITRIC OXIDE • General inhalation • Changes membrane thickness à • Facial jaw surgery
(laughing gas) anesthesia affect gating properties of ion • Situations where local
channels in neurons anesthesia fails
• Interfere with release & re-‐uptake • Patients with physical
of NTs at post-‐synaptic terminals health problems
and/or alter conductivity of ions • Mental retardation
after receptor is activated by a NT • Phobic patients
• Activates GABA receptors
hyperpolarizing cell membranes
• Inhibit impulse transmission from
neuron to neuron in CNS

SEVOFLURANE • General inhalation • See nitric oxide • See nitric oxide • Most frequently used
anesthesia inhalation anesthetic
• Rapid onset & clearance
• Non-‐irritant
• Side effects:
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-‐ Cough, interrupted
breathing,
bradyarrhythmia

DESFLURANE • General inhalation • See nitric oxide • See nitric oxide
anesthesia

ISOFLURANE • General inhalation • See nitric oxide • See nitric oxide • Isomer of enflurane
anesthesia • Slightly more potent
• Induction dose 1.5-‐3%
• Maintenance 1-‐2%

PROPOFOL • Sedative hypnotic • Increased activity of GABA by • Induction & • No analgesic effects
agent interacting with GABA A receptor maintenance of • Fast onset, very fast recovery
complex at spinal & supra-‐spinal anesthesia • Induces hypnosis with
synapses à CNS depression à • Sedation in critical minimal excitation (within 40
from light sleep to deep coma care settings seconds from injection)
(dose dependent)

BENZOCAINE • Ester type anesthetic • Block initiation & conduction of • Infiltration & regional • Metabolized to p-‐
• Short acting nerve impulses by decreasing anesthesia in patients aminobenzoic acid à allergic
(hydrolzed rapidly by neurons permeability to Na+ ions with amide allergy • Due to toxicity + allergy à
butyryl à inhibits depolarization à AP • Short acting esters have limited use
cholinesterase) not conducted • Local pain on soft • Pregnancy à category C à
tissues (e.g. throat avoid
pain) as tablets

TETRACAINE • Ester type anesthetic • See benzocaine • See benzocaine • Pregnancy à category C à
• Short acting avoid
(hydrolyzed)

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LIDOCAINE • Amide type • blocks Na+ channels in heart • acute treatment of • NOT metabolized to p-‐
anesthetic muscle ventricular aminobenzoic acid à very
• Short acting (NOT • suppresses automaticity of arrhythmias rarely allergic
hydrolyzed) conduction tissue (increasing • local & regional • Can be used in pregnant
• 1B anti-‐arrhythmic threshold of ventricle) anesthesia (Category B; + Prilocaine)
agent • spontaneous depolarization of (infiltration, nerve
• no pill à i.v. or i.m. ventricles during diastole block, epidural, spinal
• also see benzocaine methods)

ARTICAINE • Amide type • See benzocaine • Local anesthetic used • NOT metabolized to p-‐
anesthetic for infiltration & aminobenzoic acid à very
• Short acting (NOT nerve blocks rarely allergic
hydrolyzed) • Rarely associated with
methemoglobinemia

MEPIVACAINE • Amide type • See benzocaine • Local anesthetic used • NOT metabolized to p-‐
anesthetic • Smallest vasodilator activity for infiltration & aminobenzoic acid à very
• Short acting (NOT nerve blocks rarely allergic
hydrolyzed) • Pregnancy à category C à
avoid
BUPIVACAINE • Amide type • See benzocaine • Local anesthetic used • NOT metabolized to p-‐
anesthetic for infiltration & aminobenzoic acid à very
• Long acting (NOT nerve blocks rarely allergic
hydrolyzed) à 5-‐10 • Pregnancy à category C à
hours! avoid

SEDATIVE & ANXIOLYTIC
AGENTS

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ALPRAZOLAM • Benzodiazepine • Binds to GABA A receptor (Cl-‐ ion • Short-‐term relief • Weaker & short action than
derivative channel; Ω1 & Ω2 à BZD1 & anxiety other BZD
• Anxiolytic BZD2) in neuronal membranes in • Panic disorder • Weak/almost no effect on
• Daily tranquilizer CNS à activated by GABA à (with/without skeletal muscle
• Intermediate acting increased neuronal membrane agoraphobia) • No sedative/hypnotic activity
(13-‐15hrs) permeability to chloride ions à • Anxiety due to • NOT against seizures
hyperpolarization + stabilization depression
• BZD potentiate GABAergic • Prior to surgery
inhibition at all levels of neuraxis • Only anxiety
(spinal cord, hypothalamus,
hippocampus, substantia nigra,
cerebellar & cerebral cortex)

DIAZEPAM • Benzodiazepine • See alprazolam • General anesthesia • All BZD potentiate alcohol
derivative • Epilepsy à all BZD derivatives can induction effects!
• Long acting (40hrs) be used (except alprazolam) à • Anxiety
bind to BZD 2 (myorelaxant) • Seizure attacks
• Anti-‐convulsant effect

MIDAZOLAM • Benzodiazepine • See aplrazolam • General anesthesia • Works against muscle
derivative induction spasms, epilepsy, seizure
• Short-‐acting (2hrs) • Pre-‐medication agent
• Short procedures
during operation
under LA
TRIAZOLAM • Benzodiazepine • See alprazolam • General anesthesia
derivative induction
• Short-‐acting (2hrs) • Pre-‐medication agent
• Short procedures
during operation
under LA
• Sleep induction
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BROMAZEPAM • Benzodiazepine • See alprazolam • Anxiety

derivative • Overwhelming stress
• Anxiolytic

BUSPIRON • 5-‐HT receptor agonist • unknown mechanism of action • short term relief of • no risk of physical
• anxiolytic agent • high affinity for serotonin anxiety dependence/withdrawal
receptors (5-‐HT 1A) • overwhelming stress symptoms
• moderate affinity for brain
dopamine (D2) receptors
• no effect on GABA binding

PHENOBARBITAL • barbiturate • binds to GABA A-‐receptor à • seizure disorders
• anxiolytic, sedative, increased GABA receptor-‐ (tonic-‐clonic, partial)
hypnotic, anti-‐ mediated ion flow by prolonging • Insomnia & anxiety
convulsant agent opening of Cl-‐ channels à drug withdrawal
• long-‐acting hyperpolarization • Surgery
• decreased excitatory responses • Hyperbilirubinemia in
(effects glutamate release) à neonates
increase of inhibitory processes & • Cholestasis
diminution of excitatory
transmission à hypnotic + anti-‐
convulsant effect

LEONURI CARDIACA • Sedative agent • sedative • panic, stress,
• Herbal (drops) insomnia
• freely available in
pharmacy

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VALERIANA • sedative agent • sedative • panic, stress,
OFFICINALIS • herbal (drops) insomnia
• freely available in
pharmacy

ZOLPIDEM • Benzodiazepine • See alprazolam • Insomnia only • Less abuse potential
analogue • Binds selectively only to BZD 1 • Minimal residual effects on
(Ω1) receptor à hypnotic effect psychomotor & cognitive
functions

ZOPICLONE • Benzodiazepine • See alprazolam • Insomnia only
analogue • Binds selectively only to BZD 1
(Ω1) receptor à hypnotic effect

ANTI-‐DEPRESSANTS

AMITRIPTYLINE • TCA (tricyclic • Serotonin & norepinephrine • major depressive, • Metabolized to notriptyline
antidepressant) reuptake inhibitor (inhibits eating, bipolar (more potent NE RI)
• Co-‐analgesic membrane pump) disorder • Contraindicated in glaucoma
• Sedative agent • Histamine, ⍺1, muscarinic • ADHD • 1/8 as potent as atropine
receptor antagonist • Anxiety (anticholinergic)
• σ1 receptor agonist à decreased • Migraine • Side effects:
apathy, psychomotor activity, • Insomnia -‐ Weight gain,
sedation, increased mood, • Prophylaxis migraine constipation, xerostomia,
• Postherpetic NMS, hepatotoxic,
neuralgia arrhythmia, MI, prolong
QT, sudden cardiac
death, sedation

19
CITALOPRAM • Antidepressant • Inhibition of CNS neuronal • Major depressive • Almost no sedative effect,
• Selective serotonin-‐ reuptake of serotonin (5-‐HT) à disorder tiredness, lack of
reuptake inhibitor more serotonin to remain in • Generalized anxiety concentration
(SSRI) synaptic cleft where it then binds disorder • Does nit potentiate alcohol
to receptors à potentiation of effect
serotonergic activity in CNS • Side effects:
-‐ Headache, nausea,
depression, worsening,
suicidal thoughts, suicide

FLUOXETINE • See citalopram • See citalopram • See citalopram + OCD • Less abuse potential
• Minimal residual effects on
psychomotor & cognitive
functions

PAROXETINE • See citalopram • See citalopram • Major depressive, • Almost no effect on other
OCD, panic, NTs
premenstrual • Less sedating than most
dysphoric disorders other antidepressants
• Social phobia • Risk of suicidal tendencies,
• PTSD sexual dysfunction,
• Premature ejaculation constipation, diarrhea, dry
• Diabetic neuropathy mouth, nausea, NMS
• Chronic headache
SERTRALINE • See citalopram • See citalopram • Major depressive, • Relatively quick onset (1
• Very weak effects on NE and D OCD, panic, week)
uptake premenstrual • Side effects:
dysphoric, social -‐ Insomnia
phobia disorders -‐ Headache
• PTSD -‐ Diarrhea
• Premature ejaculation -‐ Nausea
20
• Diabetic neuropathy -‐ Vomiting
• Vascular headache
DULOXETINE • Antidepressant, • Inhibition of CNS neuronal • Major depressive,

anxiolytic agent reuptake of serotonin 5-‐HT (more) generalized anxiety
• Selective serotonin & NE (less) à potentiation of disorder
NE reuptake inhibitor serotonergic & noradrenergic • Neuropathic pain
(SNRI) activity in CNS à antidepressant • Fibromyalgia
• Co-‐analgesic & anxiolytic effects • Stress
• Potentiation of serotonin & NE in • Urinary incontinence
sacral spinal cord à increased
urethral closure à reduction of
involuntary urine loss

VENLAFAXINE • Antidepressant, • Inhibition of CNS neuronal • Major depressive, • Can increase BP
anxiolytic agent reuptake of serotonin 5-‐HT (more) generalized anxiety • Side effects:
• Selective serotonin & NE (less) à potentiation of disorder -‐ Weight loss
NE reuptake inhibitor serotonergic & noradrenergic • Social phobia -‐ Hypertension
(SNRI) activity in CNS à antidepressant • Panic disorder -‐ Xerostomia
& anxiolytic effects -‐ Sweating symptom
• Weak inhibition of dopamine -‐ Nausea
-‐ Hepatitis

ANTI-‐PSYCHOTICS

HALOPERIDOL • Typical antipsychotic • Competitive blockade of post-‐ • Schizophrenia • High risk of EPS, QT interval
agent synaptic D2 receptors in • Acute psychoses elongation, NMS* EPS
• High-‐potency mesolimbic dopaminergic system • Hyperactivity reduced by trihexyphenidyl
butyrophenone • Increases turnover of brain • Alcohol delirium • Weak adrenoblocking activity
dopamine à produce its • Antiemetic • no anti-‐muscarinic activity
21
tranquilizing, antipsychotic, anti-‐ • Strongly sedative • long half-‐life (15-‐40h)
emetic effects
• Potentiates analgesic agents’
effects
* blockade in tuberoinfundibular
system à decreased growth hormone
release; increased prolactin release in
pituitary gland
OLANZAPINE • Atypical antipsychotic • Antagonism of 5-‐HT 2A+2C, D1-‐4, • Schizophrenia • Can be combined with
agent H1, ⍺ 1-‐adrenergic receptors (negative symptoms, haloperidol
• Thienobenzodiazepine • Moderate antagonism of 5-‐HT 3, resistant form) • Side effects:
M1-‐5 receptors • Psychosis (e.g. -‐ Sleepiness
• Weak binding to GABA A, BZD, β-‐ alcoholic) -‐ Vertigo
adrenergic receptors à potent • Mania in bipolar -‐ Hypotonia
antipsychotic, sedative, hypnotic disorder -‐ Dry mouth
effects • Increased prolactin à
gynecomastia + galactorrhea

QUETIAPINE • Atypical antipsychotic • D2 + ⍺ 2-‐adrenergic receptor • Schizophrenia • Effective in psychic
agent antagonist • Mania in bipolar symptoms in patients with
• Dibenzozhiazepine • Weak 5-‐HT 2 receptor antagonist disorder parkinsonism
à antipsychotic, sedative,
antimanic effects
• Decreases negative and positive
schizophrenia symptoms
• Histamine negative activity

CLOZAPINE • Atypical antipsychotic • D2 + 5-‐HT 2A receptor antagonist • resistant & negative • Side effects:
agent • ⍺ -‐adrenergic, H1, cholinergic, schizophrenia -‐ Agranulocytosis
other dopaminergic, serotonergic • suicidal behavior -‐ Leukopenia
receptor broad efficacy range • negative symptoms of -‐ Constipation
schizophrenia -‐ Hypotension
22
• strong sedative effect in beginning -‐ Weight gain
of treatment • Potent central anticholinergic
• 5-‐HT 2A à negative + resistant effects (trihexyphenidyl like);
schizophrenia no EPS
RISPERIDONE • Atypical antipsychotic • Binds to 5-‐HT 2 receptor in CNS & • Long-‐term treatment
agent periphery with high affinity schizophrenia
• Bind to dopamine D2 receptors (positive & negative
with less affinity symptoms)
• CNS activating effect (low doses), • Low doses used in
antipsychotic (at higher doses) à senior patient
improves negative symptoms of dementia (psychoses
psychoses & decreases incidence & aggression)
of extrapyramidal side effects

ARIPIPRAZOLE • Atypical antipsychotic • Partial agonist at D2 & antagonist • Schizophrenia • No antimuscarinic effect
agent (new for 5-‐HT 2A receptor (positive & negative • Little risk of sides
generation) • Moderate affinity D4, 5-‐HT 2C+7, symptoms) • No EPS
• Quionoline ⍺ 1-‐adrenergic, H1 receptors • Mania (bipolar • Elevated prolactin
• Moderate affinity for serotonin disorder) • Weight gain
reuptake transporter à strong • Major depressive
antipsychotic activity disorder
• Autism
LITHIUM SALT • Antipsychotic agent • Mechanism unknown • Bipolar affective
• Mood stabilizer • Suppresses inositol signaling & disorder (mania/acute
inhibits glycogen synthase kinase -‐ mania)
3 (GSK-‐3, multifunctional protein
kinase)

23

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Colloquium Paula Swiontek

NIMESULIDE • NSAID • Weakly inhibits COX2 à • Acute pain, • Hepatotoxic!

BROMAZEPAM • Benzodiazepine • See alprazolam • Anxiety

DULOXETINE • Antidepressant, • Inhibition of CNS neuronal • Major depressive,

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