Introduction pharmacology Flashcards

1
Q

Drug producing 50% of maximum clinical effect?

A

Effective concentration (EC50)

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2
Q

Drug producing 50% of maximum clinical effect in 50% of subject?

A

Effective dose (ED50)

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3
Q

Drug dose required to produce a toxic effect in 50% of subject?

A

Toxic dose(TD50)

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4
Q

Drug dose causing death in 50% of subject?

A

Letha; dose(LD50)

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5
Q

dose of drug will be between ED50 and TD50?

A

Therapeutic window

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6
Q

What does ionized (H2O soluble) does to the absorption?

A

Decrease absorption

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7
Q

What does unionized (lipid soluble) does in the body?

A

Increase absorption

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8
Q

Is Ka inversely proportional to pKa?

A

yes

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9
Q

Increase in ka causes complete or partial dissociation?

A

complete dissociate

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10
Q

Are ionized in acidic conditions

A

Basic drugs

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11
Q

Are ioniozed in basic conditions

A

Acidic drugs

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12
Q

HA mean?

A

acid unionized

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13
Q

A- mean?

A

acid ionized

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14
Q

B means

A

base unionized

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15
Q

HB+ means

A

base ionized

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16
Q

What are the families of receptors?

A

Ligand-gated ion channels
G-protein coupled receptors
Enzyme linked receptors
intracellular receptors

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17
Q

Decrease in pH cause acidity to?

A

increase

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18
Q

Increase in Ka causes acidity to?

A

increase

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19
Q

decrease in pka causes acid to?

A

increase

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20
Q

Example of ligand-gated ion channels are?

A

cholinergic nicotinic receptor

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21
Q

ligand-gated ion channel causes:

A

cell membrane
neurotransmission
muscle contraction

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22
Q

In G-protein coupled receptor, GDP switches to?

A

GTP

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23
Q

When the drug/ligand binds to GPCR what does it triggers?

A

phosphorylation

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24
Q

WHat subunit binds to gtp to cause cellular response?

A

alpha

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25
Q

WHat is the example of GPCR

A

alpha adrenergic receptors

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26
Q

Example of enzyme-linked receptor?

A

insulin receptor

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27
Q

Which enzyme is involved in enzyme-linked receptor?

A

tyrosine kinase

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28
Q

once tyrosine kinase is ______ it triggers response

A

phosphorylated

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29
Q

Example of intracellular receptors:

A

steroid
thyroid
nuclear receptor

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30
Q

What does intracellular receptors do?

A

targets DNA to cause gene modification

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31
Q

Ocuurs when one signalling molecule produces changes in thousands of proteins

A

Signal amplification

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32
Q

drug binds to receptor?

A

Affinity

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33
Q

drug produces clinical response

A

potency

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34
Q

Increase in potency cause __ in drug concentration

A

decrease

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35
Q

drug to produce response during interaction with receptor

A

efficacy

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36
Q

drug-receptor complex to prduce maximal clinical effect

A

intrinsic activity

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37
Q

ability of 1 drug molecule to interact with 1 receptor to produce response

A

intrinsic efficacy

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38
Q

What are the 4 types of drug interaction?

A

Synergism
Addition
potentiation
antagonism

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39
Q

This drug interaction means combination drug has greater effect than individual drugs (Effect Ab» Effect A + effect of B)

A

Synergism

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40
Q

This drug interaction means one drug increases the effect (or protects the) of another drug.

A

potentiation

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41
Q

Example. of potentiation

A

Levodopa+carbidopa and amoxicillin+clavulinic acid

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42
Q

This drug-receptor interactions activates the receptor?

A

Agonist

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43
Q

This drug-receptor interactions inhibits/attenuates agonist effect?

A

antagonist

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44
Q

produces Full effect

A

Full agonist

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45
Q

does not produce 100% activation

A

partial agonist

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46
Q

produces opposite effects of the agonist and effect is below the baseline

A

inverse agonist

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47
Q

Example of inverse agonist

A

anti-histamines

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48
Q

drugs binds to agonistis receptor site, can be overcome by increase in agonist

A

competitive inhibition

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49
Q

drug binds to allosteric site

A

non-competitive inhibition

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50
Q

Reversible antagonist can be reversed with increase in?

A

substrate

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51
Q

Produces lower effect after prolong use of drug same dose

A

Downregualtion

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52
Q

Example of downregulations are”

A

opoids
alcohol
nicotine

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53
Q

Produces higher effect after prolong use with same dose?

A

supersensitization

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54
Q

example of supersensitization

A

antipsycotic drugs

dyskinesia

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55
Q

send signals from BRAIN to ORGANS

A

Efferent

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56
Q

send signals from ORGANs to BRAIN

A

Afferent

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57
Q

This ANS nerve has long preganglionic nerve and short postganglionic nerve?

A

Parasympathetic

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58
Q

In parasympathetic system postganglionic nerve Ach binds to which receptor

A

Muscarinic receptor

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59
Q

This system also known as rest and digest

A

Parasympathetic

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60
Q

This ANS system responses to emergency situation

A

sympathetci

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61
Q

In this ANS system has NE at posganglionic nerve and binds to :

A

sympathetic and binds to alpha and beta

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62
Q

Is the origin of sympatheic nerve?

A

thoracolumbar

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63
Q

origin of parasympathetic nerve?

A

craniumsacral

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64
Q

This is also known as fear, fight and flight?

A

sympathetic

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65
Q

What are the sympathetic effects on Heart?

A

Increase cardiac outputs (increase in BP and HR). increase conductivity

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66
Q

What are the sympathetic effects on BV?

A

Vasoconstriction and vasodilation

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67
Q

Vasoconstrictions happens in which blood vessel?

A

skin and mucus membrane

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68
Q

vasodilation happens in which BV?

A

coronary and skeletal muscle

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69
Q

What are the sympathetic effects on Respiratory system?

A

bronchodilation

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70
Q

What are the sympathetic effects on GIT?

A

constipation and urinary retention (relaxes the sphincter)

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71
Q

What are the sympathetic effects on male sex organ?

A

ejaculation

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72
Q

What are the sympathetic effects on female sex organ?

A

relaxation of uterus

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73
Q

What are the sympathetic effects on Eyes?

A

mydriasis
far accomodation (ciliary muscles relaxes)
closes canal of schlemm (increase in IOP-glaucome)

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74
Q

What are the sympathetic effects on Exocrine glands?

A

viscous secretions causes dry mouth

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75
Q

What are the sympathetic effects on metabolism?

A

glycogenolysis
lipolysis
gluconeogenesis

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76
Q

This system control the radial muscle?

A

sympathetic

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77
Q

Parasympathetic control which muscle in the eyes?

A

circular muscle

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78
Q

Sympathetic receptors also known as:

A

Adrenergic receptors

79
Q

Example of adrenergic receptors

A

alpha and beta

80
Q

parasympathetic receptors AKA:

A

cholinergic receptors

81
Q

M1 (muscarinis 1 receptors) is responsible for:

A

cognitive

82
Q

M2:

A

smoth muscles

83
Q

Nm is

A

motor end plate of muscles

84
Q

Nn

A

ganglia and CNS

85
Q

This nicotinic receptor has role in alzheimer’s

A

Nn

86
Q

What si the effect of vagal nerve on CNS and heart?

A

slows down the heart rate (bradycardia)

87
Q

What is the orgin of sweat gland?

A

thoraculumbar

88
Q

sweat gland has this receptor at posganglia

A

Ach on muscarinic

89
Q

What are the 3ways to stop sympathetic effects?

A

MAO
COMT
Reuptake of NE

90
Q

Way to stop PS effect?

A

Acetylcholinesterase - inhibits Ach

91
Q

is an autoimmune disease where nicotinic muscular (NM) receptor is damaged

A

Myasthenia gravis

92
Q

Myasthenia gravis causes:

A

weak muscle tone

93
Q

SE of Myasthenia gravis are:

A

drooping eyelid
trouble talking
trouble walking

94
Q

What are the examples of direct acting cholinergic agonsit:

A

Choline esters

cholinomimmetic alkaloids

95
Q

Example fo choline esters:

A

Methacholine
Bethanocholine
Carbachol

96
Q

MOA of Choline esters:

A

Ach mimmetics

97
Q

this choline ester is used for post-ocular surgery

A

carbachol

98
Q

a choline ester bethanecol is used for

A

urinary retention

99
Q

a choline ester methacholine us used for

A

test for asthma

100
Q

example of direct acting cholinomimmetic alkaloids

A

pilocarpine and cevemeline

101
Q

MOA of direct actin cholinomimmetic alkaloids in mouth and eyes is:

A

induces saliva secretion

decrease IOP

102
Q

Pilocarpine is used for

A

dry mouth and glaucoma

103
Q

Example of indirect action acetylcholinesterase antagonist are:

A

reversible and irreversible

104
Q

Example of irreversible cholinesterase inhibitors are:

A

organophosphate compounds

105
Q

irreversible cholinesterase inhibitors causes:

A

Bronchospasm
salivation
lacrimation
convulsions

106
Q

Reversible cholinesterase inhibitors are belongs to which family:

A

Stigmine family

107
Q

is an antidote for atropine toxicity and passes BBB (tertiary amine)

A

physostigmine

108
Q

this drug is used for diagnosis(edrophonium) and txt for myasthenia gravis

A

neostigmine (prostigmine)

109
Q

Antidote of curare poisoning

A

neostigmine (prostigmine)

110
Q

used for post-operative urinary retention and paralytic ileus

A

neostigmine (prostigmine)

111
Q

Is used for txt of myasthenia gravis

A

pyrodostigmine and ambenonium

112
Q

used for diagnosis of myasthenia gravis and is short acting drug (5 minutes)

A

edrophonium

113
Q

These drugs are used alzheimer’s disease

A

Rivastigmine and donepezil

114
Q

This drug is the father of parasympatholytic drugs

A

atropine

115
Q

Atropine is an

A

anticholinergic and muscarinic blocker

116
Q

7 common SE of anticholinergic drugs (atropine)

A
Tachycardia
Blurred vision
photo[hobia
dry mouth
urinary retention
constipation
hallucination
excitation
fever (no sweating)
117
Q

atropine is used for:

A

mydriasis
dry secretions
organophosphate toxicity
antispasmodic

118
Q

This atropine like medication is used as atropine substitute for mydriasis and is short duration

A

homotropine and tropicamide

119
Q

Anti-parkinsons drugs are:

A

benzotropine and trihexphenidyl

120
Q

used for bronchial asthma and COPD

A

Spiriva and atrovent SE: dry mouth

121
Q

Atropine like meds that does not pass BBB:

A

Toviaz
Solifenacin
oxybutynin

122
Q

Example of direct acting sympathomimemtic agents:

A
epinephrine (alpha, beta)
NE (a)
Isoprenaline (b)
phenylprenaline (a1)
salbutamol(b2)
dobutamine(b1)
123
Q

Act by increasing the release of NE from vesicles

A

indirect acting sympathomimetic agents

124
Q

Example of indirect acting sympathomimetic agents

A

tyramine

amphetamine

125
Q

example of mixed acting sympathomimetic agents

A

ephedrine

126
Q

Example of alpha 1 agonists are:

A
Phenylephrine
xylometazoline
pseudoephedrine
ephedrine
methoxamine
127
Q

alpha 1 agonists are used for:

A

congestion
pupil dilation
hypotention

128
Q

examples of alpha 2 agonists are:

A

methyldopa and clonidine

129
Q

alpha 2 is used for:

A

hypertension

130
Q

SE of clonidine

A

rebound hypertension

131
Q

Is weak antihypertensive agent

A

clonidine

132
Q

B1 drugs are:

A

dobutamine

133
Q

B2 drugs are:

A

SABA : salbutamol, terbutaline, isoproterenol

LABA: salmeterol , formoterol

134
Q

b3 drugs are:

A

mirabegron

135
Q

b1 and b2 drugs are:

A

isopreternol

136
Q

b1 drugs are used for:

A

heart failure
bradycardia
heart block

137
Q

b2 drugs are used for:

A

asthma
copd
respiratory disease
prevents premature labor

138
Q

b3 drugs are used for:

A

overactive bladder

139
Q

b1 and b2 drugs are used for

A

bronchial asthma (only isoprenaline)

140
Q

Amphetamine like drugs are:

A
Amphetamine(dextroamphetamine)
methamphetamine
methylphenidate
tyramine
ephedrine
141
Q

amphetamine like drugs are used for:

A

narcoplesy
ADD
ADHD

142
Q

MOA of amphetamine like drugs

A

increase release of catecholamines

143
Q

SE of amphetamine like drugs

A
Anorexia
stomach upset
restlessness
increase HR and BP
elevated adrenereceptros activation
inhibits physical growth
144
Q

What are the 3 classification’s of sympatholytic drugs:

A

ARB (adrenergic receptor blocker)
ANB(adreergic neuron blocker)
CAD(centrally acting drugs)- clonidine and alpha methyl dopa

145
Q

Drugs that inhibts the NE relase

A

Guanithidine

146
Q

Drugs that inhibit NE STORAGE

A

reserpine

147
Q

drugs that inhibit NE synthesis

A

alpha methyl dopa

148
Q

5 uses of a1 blockers:

A
Prostate enlargment
Peripheral vascular disease
Phaechromycytoma
Hypertension
Erect dysfunction
149
Q

Alpha blockers belong to which family:

A

Zocine family

150
Q

Common 5 SE of a1 blockers as vasodilators:

A
Reflex tachycardia
postural hypotension
headache
flushing
congested nose
151
Q

example of a2 blocker

A

yohimbine

152
Q

non-selevtive b blockers are:

A
Nadolol
sotalol
timolol
propranolol
pindolol
153
Q

b blockers are used for:

A
Hypertenions
arrythmia
congestive heart failure
glucoma
angina (avoid non-selectiv)
154
Q

What are the types of Aneshtesia?

A

Local and General Anesthesia

155
Q

Is the reversible state of CNS that eliminates perception and response to external stimuli.

A

Anesthesia

156
Q

Stages of Anesthesia:

A

induction
Maintenance
Recovery

157
Q

General anesthesia act by?

A

increasing GABA receptor

decrease NMDA or aspartate glutamate

158
Q

GA act on?

A

inhibiting Reticular activating system (RAS)

159
Q

What are the 4 depts of Anesthesia?

A

Analgesia
Excitement
Surgical anesthesia
Medullary paralysis

160
Q

What are the two types of GA?

A

Inhaled and IV

161
Q

This type of GA is used for maintenance stage of anesthesia?

A

Inhaled GA

162
Q

Give 2 classes of Inhaled GA:

A

Nitrous oxide

Fluranes

163
Q

Give 4 classes of IV GA:

A

Propofol
ketamine
thiopental (barbiturate)
midazolam (benzo)

164
Q

What are the 5 conditions to be worried about if administering Inhaled GA?

A
CVS
Respiratory
Liver
CNS
Malignant hyperthermia
165
Q

this is the oldest member of flurane?

A

Halothane

166
Q

This is the best direct muscle relaxant but is irritant to the lungs?

A

Isoflurane

167
Q

This flurane has no odour and has less side effect compared to other members of flurane family?

A

Sevoflurane

168
Q

What causes malignant hyperthermia?

A

Halothane

169
Q

What causes neurolyptic malignant syndrome (NMS)

A

Antipsycotic drugs

170
Q

This anesthethic blocks the sodium channels.

A

Local anesthetic

171
Q

What are the 2 classes of Local anesthetics?

A

Esters

Amide

172
Q

Examples of Ester LA:

A

Benzocaine
Cocaine
Procaine
Tetracaine

173
Q

Examples of amides LA:

A

Lidocaine
Bupivacaine
Ropivacaine

174
Q

This amide causes arrythmis, bradycardia and it is the weak LA.

A

Lidocaine

175
Q

This is the strong LA:

A

Bupivacaine

176
Q

What are the pre-anesthetic medications?

A
BASAAO
Benzodiazepines
Anticholinergic
Skeletal muscle relaxant
Antihistamine
Antiemetic
Opoid analgesics
177
Q

This anticholinergic drug avoids bradycardia

A

atropine

178
Q

This preanesthetic med calms the pt.

A

Benzodiazepines (diazepam)

179
Q

What are the 3 different classes of drugs Na channel blockers?

A

Class I antiarrythmia
Anti-epileptic (carbamazepine and phenytoin)
LA

180
Q

THis is AKA Laughing gas

A

Nitrous oxide

181
Q

Nitrous oxide is commonly known as Laughing gas and as well _____.

A

incomplete anaesthesia

182
Q

80% N2O should be mixed with how much of O2 if giving as LA.

A

20%

183
Q

This IV GA is NMDA antagonist

A

ketamine

184
Q

Ketamine produces state of?

A

Dissociative anesthesia

185
Q

This IV GA drug cannot be used in pregnancy

A

Ketamine

186
Q

This peripherally acting drugs inhibits the synthesis of Ach

A

hemicholinium

187
Q

This peripherally acting drugs stops the release of Ach

A

botulinum toxin

188
Q

This competitive nerumuscular blocker (NMB) release histamine and produces flaccid paralysis as well

A

Curare

189
Q

This is the antidote of curare

A

neostigmine

190
Q

This depolarizing NMB produces spastic paralysis

A

Succinylchloride

191
Q

Succinylchloride is metabolized by

A

pseudocholinesterase

192
Q

What are the centrally acting drugs?

A

Baclofen
Tizanidine (Sirdalol)
Flexinire
Methicarbamol

193
Q

This type of skeletal muscle relaxant decreases Ca release from sarcoplasmic reticulum leading to inhibiton of muscle contraction

A

Direct -acting muscle relaxant

194
Q

This is the DOC for malignant hyperthermia and it is direct acting muscle relaxant.

A

Dantrolene