Antipsychotic agents. Anxiolitics. Pharmacy.pdf

Antipsychotics
Drugs
Pharmacology
Pharmacy
MBBS
Medical school

1. Antipsychotic agents.
Anxiolytics
Nailya Bulatova MD, PhD,
Professor of Pharmacotherapy
The University of Jordan-School of Pharmacy-
Department of Biopharmaceutics & Clinical
Pharmacy,
Amman, Jordan

2. PSYCHOTROPIC DRUGS (cont’d)
•used in mental illnesses: psychoses, neurotic &
pseudoneurotic disorders, associated with stress,
nervousness, fear, anxiety & other symptoms.
•in psychoses antipsychotic drugs (e.g.,
chlorpromazine, haloperidol, risperidone),
antidepressants (e.g., amitryptiline, citalopram) &
lithium salts are used.
•most antipsychotic drugs have also calming
(sedative) effect.
•antidepressants eliminate depression.
•nonselective MAO inhibitors (e.g., nialamide) have
psychostimulant effect.

3. PSYCHOTROPIC DRUGS (cont’d)
Group

Drugs used
mainly in
psychoses
Drugs used mainly in
psychiatric disorders of
non-psychotic nature*
Drugs with
psychosedative action
Antipsychotic
drugs
Antidepressants
Anxiolytics
Sedative drugs

Drugs with
psychostimulant action
Antidepressants

Psychostimulants

Drugs that have
neither psychosedative
nor psychostimulant
effect in healthy
person
Drugs to treat
mania (lithium
salts)


* or so-called borderline states

4. PSYCHOTROPIC DRUGS (cont’d)
•Tricyclic antidepressants (e.g., amitryptiline) also
have psychostimulant & sedative effects.
•lithium salts are used to treat & prevent manic
states; they have neither stimulating nor sedative
effect in normal person.
•in psychiatric disorders of non-psychotic (neurotic)
nature, anxiolytics (e.g., diazepam), sedatives
(bromides, valerian preparations) &
psychostimulants (sydnocarb) are used.
•psychotropic drugs also include hallucinogens or
psychotomimetics (LSD-25, mescaline, etc.) - cause
short-lasting acutely developing psychoses &
psychological dependence.

5. PSYCHOTROPIC DRUGS (cont’d)
•Discovery of psychotropic drugs has dramatically
changed management of psychiatric disorders.
•before that, treatment for such patients was extreme
(electroshock therapy & insulin coma).
•psychotropic drugs are also used in other fields of
medicine - therapy, anaesthesiology, neurology, etc.
•They also hepled to understand complex issues as
mechanisms of the higher nervous activity, aetiology
& pathogenesis of psychiatric disorders.

6. ANTIPSYCHOTIC (NEUROLEPTIC) DRUGS
1

•antipsychotic & marked sedative (calming) action.
•antipsychotic effect ↓productive symptoms of
psychoses (delusions, hallucinations) & delays
further progression of disease.
•psychosedative action: general sedation - elimination
of affective reactions, ↓ in anxiety, nervousness, &
↓in motor activity.
•MoA: most drugs (-) postsynaptic dopamine (DA) D
2-
receptors in limbic system.

1
From Greek neuron - nerve, leptos - delicate, thin.

7. ANTIPSYCHOTIC DRUGS

(cont’d)
•The main SE: extrapyramidal disorders is due to
dopaminergic effect in neostriatum.
•(-) of nigrostriatal transmission & ↓ of suppression
of striatum by substantia nigra → change of effect of
striatum on motor activity control→
•↑ activity of spinal cord α-motoneurons, ↑
muscular tone & drug-induced parkinsonism
(hypokinesia, rigidity & tremor).
•change in neostriatum is part of antipsychotic effect.
•(-) of DA receptors is also associated with other
effects.

8. ANTIPSYCHOTIC DRUGS

(cont’d)
•Sedative action of antipsychotics:
1. effect on ascending reticular formation of brainstem.
•(-) adrenoreceptors → eliminate EEG activation by
external stimuli in reticular formation.
2. effect on limbic system & hypothalamus.
•on EEG, the sedative action of antipsychotics leads to
high-voltage slow oscillations (result of EEG
synchronization).

9. I.P. PAVLOV (1849-1936). Russian physiologist, founder of objective study of
physiology & pharmacology of higher nervous activity. Author of conditioned
reflex method. Using method of conditioned reflexes, studied psychotropic effect
of caffeine, bromides & alcohol. Nobel Prize winner (1904).

10. Some effects associated with cerebral DA
receptors blockade by antipsychotics.
DA receptors localization Main effects
Mesolimbic & mesocortical
systems

Antipsychotic effect.
Emotional indifference.
Depression
Hypothalamus-hypophysis

↓ body temperature.
Galactorrhea (↑prolactin
release)
Extrapyramidal system

Parkinsonism symptoms;
delayed dyskinesia
Trigger zone of vomiting center Antiemetic effect

11. ANTIPSYCHOTIC DRUGS

(cont’d)
•For some antipsychotics (e.g., phenothiazines),
psychotropic effects are linked to blockade of
serotonin receptors & M-cholinoceptors of brain.
•antipsychotic drugs are divided into «typical» &
«atypical».
•«typical» drugs lead to extrapyramidal dysfunction
(parkinsonism & other motor disorders).
•«atypical» antipsychotics cause parkinsonism rarely
& it is mild - binding to different receptors,
particularly various subtypes of DA receptors.

12. ANTIPSYCHOTIC DRUGS

(cont’d)
Classification:
A «Typical» (1
st
generation) antipsychotics
◊ Phenothiazines
- Chlorpromazine (aminazine) - Trifluoperazine
(triftazinum) - Fluphenazine (phthorphenazinum)
◊ Thioxanthene derivatives - Chlorprothixene
◊ Butyrophenone derivatives - Haloperidol
B «Atypical» (2
nd
generation) antipsychotics
◊ Benzamides - Sulpiride
◊ Benzodiazepine derivatives - Clozapine (azaleptinum)

13. ANTIPSYCHOTIC DRUGS

(cont’d)
Lippincott

14. ANTIPSYCHOTIC DRUGS

(cont’d)
•Most antipsychotics are
phenothiazines;
depending on
N
10
radicals, are
subdivided into:
• Aliphatic
derivatives (chlorpromazine)
•Piperazines (trifluoperazin
e, fluphenazine)
•phenothiazines.

Phenothiazine structure

15. Chemical structures of some antipsychotics.

16. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Chlorpromazine (aminazine, largactil): typical
phenothiazine.
•marked effect on CNS & on peripheral innervation,
organs & metabolism.
•CNS: antipsychotic & sedative action, extrapyramidal
disorders (after long-term therapy).
•high doses: hypnotic effect: superficial sleep, easily
interrupted by external stimuli.
•muscle relaxation →↓motor activity. [(-) supraspinal
regulation of muscular tone mainly via basal ganglia].

17. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Chlorpromazine ↓or fully eliminates descending
facilitating effects of reticular formation on spinal
reflexes.
•(-) center of thermoregulation → most often
insignificant hypothermia is observed (↑ heat loss).
•if applied under low temperatures (physical cooling),
there is marked ↓body temperature.
•antiemetic effect (block of DA receptors of trigger
zone at bottom of the IVth ventricle).

18. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Chlorpromazine potentiates action of general
anesthetics, hypnotics (non selective CNS
depressants), & opioid analgesics.
•- partially because chlorpromazine (-) metabolism of
these drugs.
•peripheral effects: α-adrenoblocking →↓pressor
reaction to epinephrine (epinephrine reversal).
•some M-cholinoceptor blocking (atropine-like) effect
→ mild suppression of salivary, bronchial & digestive
gland secretion.

19. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Chlorpromazine has local anesthetic effect on topical
application.
•antihistamine activity (blocks histamine H
1-
receptors).
•spasmolytic of myotropic action.
•cardiovascular effects: ↓ arterial BP by: 1. (-) of
hypothalamic centers, 2. α-adrenoceptor blocking
effect, 3. spasmolytic effect, 4. (-) of compensatory
vasoconstrictive reflexes, 5. ↓force of cardiac
contractions.
•hypotension → reflex tachycardia.

20. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Chlorpromazine is PO & parenterally.
•duration of effect ~6 h.
•IV injection should be slow.
•tolerance can develop after long-term therapy to
sedative, hypotensive & some other effects;
•no tolerance to antipsychotic action.

21. Pharmacokinetics of some antipsychotics
Drug

Bioavaila
bility
(oral
route),%

Time to peak
plasma
concentration
, h
Binding to
plasma
proteins,
%

Plasma
half-life
(t
1/2)
h



Renal
excretion,
%

Chlorpromazin
e
(aminazinum)
15-50

1-4

95-98

25-35

<1

Phthorphenazi
ne
1.7-4.5

1-4

0

8-16

<1

Haloperidol 40-80 0.5-0.7 90-94 12-23 ~1
Clozapine 43-67 1.1-2.7 >95 8-16 <1
Risperidone 40-90 ~1 ~90 2.4-4* 1-5
* t
1/2 of active metabolite - 20-24 h.

22. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Compounds, that have piperazine in side chain,
bound with phenothiazine nitrogen atom:
trifluoperazine, fluphenazine, etc.
•Trifluoperazine (triftazine, stelazine): > selective
antipsychotic effect than chlorpromazine & < marked
sedative effects.
•> antiemetic than chlorpromazine.
•weaker hypotensive, α-adrenoceptor blocking &
muscle relaxing effects.
•Extrapyramidal disorders (EPDs) occur > often.

23. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Fluphenazine (phthorphenazinum, moditen): similar
to trifluoperazine in antipsychotic efficacy.
•> antiemetic than trifluoperazine.
•fluphenazine decanoate (moditen-depot) (IM) acts
for 7-14 days & >.
•phenothiazine SEs: general weakness, apathy,
drowsiness, dry mouth & discomfort in heart &
epigastrum.
•hypotension, orthostatic collapse may occur
(common with chlorpromazine).

24. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•(phenothiazine SEs): sometimes obstructive jaundice
(usually with chlorpromazine).
•EPDs (parkinsonism, etc.) are typical for
phenothiazines).
•after long-term (months or years) therapy with
phenothiazines, tardive dyskinesia
1
: involuntary
choreoathetoid contractions of facial muscles,
tongue, extremities & other skeletal muscles - most
often in elderly patients.

25. ANTIPSYCHOTIC DRUGS

(cont’d)
•Video Tardive dyskinesia:
https://www.youtube.com/watch?v=FUr8ltXh1Pc
•In such cases antipsychotic drug is usually
discontinued or its dose is reduced.
•(in some cases ↑ dose ↓ dyskinesia manifestations).
•any concomitant drugs with M-cholinoceptor
blocking activity (antidepressants, antiparkinsonian
drugs) should be discontinued.
•sometimes diazepam is used.
•tardive dyskinesia may be also caused by
butyrophenone & thioxanthene derivatives.
•atypical antipsychotics cause this effect much <.

26. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•malignant neuroleptic syndrome: idiosyncratic
reaction to drug.
•muscular rigidity appears, body temperature
abruptly ↑, cardiovascular function is disturbed,
consciousness is impaired, etc.
•~ 10-20% of such patients die.
•treatment: diazepam, bromocriptine & dan-trolene
2
.
•
2
dantrolene causes muscle relaxation, affecting
sarcoplasmic reticulum & preventing Ca
2+
ion
release.
•external physical cooling is also performed.

27. ANTIPSYCHOTIC DRUGS: Phenothiazines

(cont’d)
•Dyspepsia, such as loss of appetite & nausea.
•irritation of skin & mucous membranes.
•can occur at places of drug administration (vein,
muscle, GIT).
•skin photosensitization, may occur.
•leukopenia & agranulocytosis (rare).

28. ANTIPSYCHOTIC DRUGS: (cont’d)
•Chlorprothixene (truxal): thioxanthene derivative.
•as antipsychotic, inferior to phenothiazines.
•has some antidepressant activity.
•marked sedative effect
•antiemetic properties
•intensifies effect of general anesthetics, hypnotics
(non-selective CNS depressants) & opioid analgesics.
•slightly inhibits α-adrenoceptors.
•SEs: similar to chlorpromazine, but skin
photosensitization & pigmentation are very rare.

29. ANTIPSYCHOTIC DRUGS: (cont’d)
•Haloperidol (halophen): butyrophenone.
•action starts relatively quickly & lasts for long time.
•high antipsychotic activity is combined with
moderate sedative effect.
•MoA: DA receptor block, central α-adrenoceptor
block, disturbance of neuronal uptake & storage of
NE.
•low doses (-) D
2-receptors of vomiting center trigger
zone.
•potentiates action of general anesthetics, hypnotics
(non-selective CNS depressants) & opioid analgesics.

30. ANTIPSYCHOTIC DRUGS: (cont’d)
•Unlike phenothiazine, haloperidol does not shorten
«fast» sleep phase.
•slightly (-) peripheral α-ARs.
•usually no ↓arterial BP & no orthostatic
hypotension.
•SE: EPDs are the most common.
•skin reactions may occur.
•leukopenia rarely develop.
•in overdose, anxiety, fear & sleeplessness appear.

31. ANTIPSYCHOTIC DRUGS: (cont’d)
•Droperidol: butyrophenone derivative.
•short-term action.
•mainly administered for neuroleptanalgesia (in
combination with analgesics).
•«atypical» antipsychotic drugs: sulpiride, clozapine,
risperidone.

32. ANTIPSYCHOTIC DRUGS: (cont’d)
•Sulpiride: substituted benzamide.
•selective blocker of D
2-receptors; substantial
antipsychotic activity.
•antiemetic action.
•insignificant sedative effect.
•slight hypotension may occur.
•EPDs are mild.
•Clozapine (leponex, azaleptinum): dibenzodiazepine
derivatives.
•high affinity to D
4-receptors (frontal cortex, amygdala
& midbrain), D
2-receptors & serotonin 5-HT
2A-
receptors.

33. ANTIPSYCHOTIC DRUGS: (cont’d)
•Clozapine (-) M-cholinoceptors & α
1-ARs of the brain.
•high antipsychotic activity.
•initially can cause sedation, which soon passes.
•< often causes EPDs, including delayed dyskinesia,
than most other antipsychotic drugs
•does not affect prolactin production.
•can be effective in patients resistant to «typical»
antipsychotic drugs.
•use should be accompanied by control of peripheral
blood (risk of agranulocytosis).

34. ANTIPSYCHOTIC DRUGS: (cont’d)
•SEs of clozapine: hypotension, HA, dizziness,
hypersalivation, weight gain & clonic-tonic seizures.
•relatively rarely used due to possible effect on
leukopoiesis.
•Risperidone: benzisoxazole derivative.
•blocks both D
2- & 5-HT
2A-receptors.
•marked antipsychotic efficacy.
•low doses – no EPDs.
•SEs: hypotension, sleeplessness, dyspeptic disorders
& allergic reactions.

35. ANTIPSYCHOTIC DRUGS: (cont’d)
•Antipsychotics are used:
• in psychoses (especially with marked excitation,
affective reactions, aggressiveness, delirium,
hallucinations).
•in complex with other drugs when treating drug
dependence (e.g., to opioid analgesics & ethyl
alcohol).
•phenothiazines & butyrophenones: as antiemetics &
in persistent hiccups.
•to potentiate action of general anesthetics, hypnotics
(non-selective CNS depressants) & opioid analgesics.

36. ANTIPSYCHOTIC DRUGS: (cont’d)
•long-term therapy with most antipsychotics
→tolerance.
•No drug dependence.
•Contraindications: or caution in liver, kidney or
active cardiovascular diseases, organic diseases of
CNS & hemopoiesis disorders.

37. ADRs PRODUCED BY ANTIPSYCHOTIC DRUGS:
(cont’d)
Lippincott

38. ANXIOLYTICS
1
(TRANQUILIZERS)
2

•
1
From Latin anxius - anxious, fearful, be crept over
by fear, Greek lysis - dissolution.
•Anxiolytics are sometimes also called ataractics (from
Greek ataraxia - coolness, peace of mind), minor
tranquilizers, as well as psychosedative,
psychostabilizing & antineurotic drugs.
•
2
From Latin tranquillium - tranquility, peace.

39. ANXIOLYTICS

(cont’d)
•anxiolytic (tranquilizing) effect → internal tension,
elimination of nervousness, anxiety & fear.
•most anxiolytics have sedative action.
•mainly used in neurotic & pseudoneurotic (reactive)
conditions.
•most drugs (except benactyzine) do not affect
autonomic innervation;
•do not induce extrapyramidal disorders.

40. ANXIOLYTICS

(cont’d)
Anxiolytics are divided into:
• Agonists of benzodiazepine (BDZ)
receptors (diazepam, phenazepamum, etc.)
• Agonists of serotonin receptors (buspirone)
• Drugs of different action types (benactyzine, etc.).
•BDZs: the most widely used.
•Duration of their action depends on presence of both
main drug & metabolite.

41. ANXIOLYTICS

(cont’d)
Classification of BDZs by duration of action:
• Long-acting (t
1/
2 = 24-48 h) – Phenazepamum
- Diazepam (sibazonum, seduxen, valium)
- Chlordiazepoxide (chlozepidum, elenium)
• Medium- acting (t
1/
2 = 6-24 h) - Nozepam (oxazepam,
tazepam) – Lorazepam - Alprazolam
• Short- acting (t
1/
2 <6 h) - Midazolam (dormicum)
Typical BDZ effects: - anxiolytic, - sedative, - hypnotic, -
muscle-relaxant, - anticonvulsive, - amnestic.

42. Chemical structures of some anxiolytics.

43. ANXIOLYTICS

(cont’d)
•BDZ psychotropic action is mainly associated with
effect on limbic system: ↓ spontaneous activity of
hippocampal neurons > hypothalamus > activating
reticular formation of brainstem.
•(+) BDZ receptors →allosteric activation of GABA
A-
receptors
•↑channel opening rate for Cl
-
→↑inward current of
Cl
•→hyperpolarization of membrane & (-) of neuronal
activity takes place.

44. Localization of action of BDZs & their antagonist flumazenil. BD
- BDZ compound with GABA-mimetic activity.

45. ANXIOLYTICS

(cont’d)
•Phenazepamum: > active than diazepam in anxiolytic
& hypnotic actions.
•BDZs with marked anxiolytic action & none or
minimal sedative-hypnotic action - «day-time
anxiolytics», e.g., medazepam (mezapamum,
rudotel).
•BDZs cause muscle relaxation (↓spinal polysynaptic
reflexes & disturb its supraspinal regulation ( central
muscle relaxants).
•anticonvulsant activity.
•high doses: amnesia.

46. ANXIOLYTICS

(cont’d)
•BDZs potentiate CNS inhibition caused by drugs with
non-selective CNS depressants action.
•in therapeutic doses do not affect arterial pressure.
•BDZs are lipophilic → easily pass through BBB.
•Rate of GI absorption: diazepam > alprazolam &
midazolam > nozepam & lorazepam.
•Some BDZ metabolites have marked & long-term
anxiolytic effect, e.g., metabolite of chlordiazepoxide
& diazepam N-desmethyldiazepam (nordiazepam),
half-life (t
1/2) of which is 40-200 h.

47. Main pathways of BDZs metabolism.

48. ANXIOLYTICS

(cont’d)
•Most BDZs & their metabolites bind with plasma
proteins (70-90%).
•high lipophility → deposition in fatty tissues.
•kidneys are main elimination route for metabolites,
conjugates (glucuronides) & small amounts of
unchanged drugs.
•well tolerated.
•SEs: drowsiness, delayed motor responses, memory
impairment, weakness, diplopia, HA, N&V,
dysmenorrhea, impotence & skin rashes.

49. ANXIOLYTICS

(cont’d)
•long-term BDZs (~6 months): tolerance; drug
dependence (psychological & physical) may occur.
•withdrawal syndrome: < severe than with BARBs.
•Flumazenil: a specific antagonist of BDZs.
•blocks BDZ receptors & eliminates or ↓intensity of
most central effects of BDZs.
•used to eliminate residual effects of BDZs (e.g., in
during surgery or for diagnostic procedures), & in
overdose or acute poisoning.
•used IV (signif. first-pass effect).
•short-term effect of 30-60 min. → may be repeated.

50. Pharmacokinetics of some BDZ anxiolytics.
Drug

Bioavailabilit
y after oral
administrati
on, %
Time to peak
plasma
concentratio
n, h
Binding
with
plasma
proteins,
%
Some active
metabolites (& their
t
1/2
,
h)

Total
duration
of effect,
h

Diazepam

90-100

1-1.5

97-99

Desmethyl-
diazepam (40-120)
24-48

Flurazepam

* 0.5-1

~97

Desalkyl-flurazepam
(47-100)
24-48

Alprazolam 75-100 0.5-3 ~70 - ~24
Clonazepam 70-100 1.5-3 ~86 - ~24
Lorazepam 90-100 1.2-2.6 ~90 - 12-18
Nitrazepam 54-98 2-3 ~87 - 18-24
Nozepam ≤100 1-4 ~97 - 12-18
Temazepam ≤100 1-2 ~96 - 12-18
* Flurazepam enters systemic circulation as active metabolites.

51. ANXIOLYTICS

(cont’d)
•Buspirone: agonist (partial) of (5-HT
1A) receptors .
•5-HT
1A are
somatodendritic: autoinhibitory effect,
→↓activity of dorsal raphe nucleus neurons & ↓
serotonin synthesis & release.
•also weak antidopaminergic activity.
•marked anxiolytic activity (close to that of diazepam).
•effect develops slowly (over 1-2 weeks).
•no sedative, anticonvulsive & muscle-relaxing action.
•low tendency for tolerance & drug dependence.
•SEs: nervousness, dizziness, HA, paraesthesias,
nausea & diarrhea.

52. ANXIOLYTICS

(cont’d)
Anxiolytics with different MoA:
•Diphenylamine derivative benactyzine (amizilum):
central cholinoceptor blockers.
•sedative effect due to (-) of M-cholinoceptors of
cerebral reticular formation.
•benactyzine ↑ effect of non-selective CNS
depressants & opioid analgesics.
•anticonvulsant activity.
•(-) cough reflex.

53. ANXIOLYTICS

(cont’d)
•Benactyzine: peripheral M-cholinoceptor blocking
action (< than central).
•→↓spasms of smooth muscles, dilates pupils & (-)
inhibits glandular secretion.
•local anesthetic & antihistamine (H
1-blocking) effect.
•SEs: atropine-like (dry mouth, tachycardia, pupillary
dilatation, etc.).
•contraindicated in glaucoma.

54. ANXIOLYTICS

(cont’d)
•Trioxazine, benzoclidine (oxylidinum) & β-
adrenoblockers also belong to anxiolytics.
Anxiolytics are mainly used in:
•treatment of neuroses & neurosis-like conditions.
•premedication before surgical interventions.
•widely in treatment of insomnia.
•BDZs in status epilepticus (IV),
•neurological disorders with ↑ tone of skeletal
muscles.
•patients who drive should not be administered BDZs
as outpatient therapy.

55. ANXIOLYTICS

(cont’d)
Future > selectively acting anxiolytics:
•cholecystokinin antagonists,
•drugs affecting serotoninergic system
•drugs interacting with excitatory amino acid
receptors.

56. SEDATIVES
•bromide salts (bromides), valerian & motherwort.
•have moderate calming action.
•bromides: sodium bromide & potassium bromide.
•↑ inhibitory processes in brain cortex.
•effect depends on type of nervous system & its
functional state.
•in «weak type» of higher nervous activity lower
doses are necessary than in higher nervous activity
of «strong type».
•marked effect in neuroses.
•Have weak antiepileptic activity.

57. SEDATIVES (cont’d)
•Bromides are distributed in body in a way similar to
chlorides (mainly extracellular distribution).
•kidneys eliminate most of drug; sweat & mammary
glands also eliminate bromides.
•half-life ~12 days.
•used in neuroses, increased irritability &
sleeplessness.
•very rarely used as antiepileptic drugs (when other
drugs are not available or as one of components in a
combined therapy).

58. SEDATIVES (cont’d)
•Due to slow elimination bromides cumulate & can
cause chronic poisoning - bromism:
•general lethargy, apathy, memory disorder; skin
lesions (acne bromica).
•irritating action → inflammation of mucous
membranes → cough, rhinitis, conjunctivitis &
diarrhoea.
•treatment of bromism: discontinuation of bromide
intake, ↑excretion in urine by large amounts of
sodium chloride, by drinking a lot of water, & by
diuretics (saluretics).

59. SEDATIVES (cont’d)
•Valerian preparations (tincture, infusion, extract):
widely used sedatives.
•obtained from rootstock & roots of common
valerian (Valeriana officinalis), which contain volatile
essential oil, valerenic acid, etc.
•Preparations of motherwort herb (tincture,
infusion), produced from quinquelobate
motherwort (Leonurus quinquelobatus) & cardiac
motherwort (Leonurus cardiaca), contain volatile
essential oil, alkaloids, saponins & tannins.

60. THANK YOU