Apraclonidine
A
131
morphine Apomorphine
CH3
Reference(s):
Small, L. et a].:
J.
Org. Chem. (JOCEAH)
5,
334 (1940).
Formulation(s):
amp. 10 mg; inj. sol. 10
mg/l
ml,
5
mg/l ml; tabl. 3 mg
Trade Name(s):
F:
Apokinon (Aguettant)
I:
Apomor (Tariff.
GB: Brilagel (Britannia; as Integrativo; as
hydrochloride) hydrochloride)
Apraclonidine
(Aplonidine)
ATC: SOlEA03
Usc: selective q-agonist (for postsurgical
control of intraocular pressure)
RN: 6671 1-21-5 MF: CyHl,,Cl,N4 MW: 245.1 1
CN:

2,6-dichloro-N1-2-imidazolidinylidene-1,4-benzenediamine
monohydrochIoride
RN: 7321 8-79-8
MF:
CYH,,C1,N4. HC1 MW: 281.57
LD,,: 6 mglkg (M, i.v.); 3 mglkg (M, p.0.);
9
mglkg (R, i.v.); 38 mglkg (R, p.0.)
dihydrochIoride
RN:
73217-88-6 MF: C9H,,Cl,N4
.2HCI
MW: 318.04
2.6-dichloro-4
nitroaniline
CI
S0Cl2. 5O2CI2
I
2.
NH,
thionyl chloride.
CC13
1.ethylenediomine
sulfuryl chloride
H
N-[4-(dichlaromethylene-
amino)-3.5-dichloro-
phenyl]trichloroacet-
omide
Referencefs):

EP 81 924 (Alcon; appl. 19.1 1.1982; USA-prior. 20.1 1.1981).
EP 81 923 (Alcon; appl. 19.11.1982; USA-prior. 20.1 1.1981).
US 4 461 904 (Alcon; 24.7.1984; prior. 20.11.198 1).
Ronot, B.; Leclerc, G.: Bull. Soc. Chim. Fr. (BSCFAS)
Pt.
2,520 (1979).
combination with P-receptor antagonist:
EP 365 662 (Alcon; 26.4.1989; USA-prior. 26.4.1988).
preparation
of
2,6-dichloro-4-nitroaniline:
Goldschmidt; Strohmenger: Ber. Dtsch. Chem. Ges. (BDCGAS) 55,2455 (1922).
Pausadeer; Scroggie: Aust. J. Chem. (AJCHAS) 12,430,432 (1959).
Fluerscheim: J. Chem. Soc. (JCSOA9)
93
1774 (1908).
Datta; Miiller: J. Am. Chem. Soc. (JACSAT) 41, 2036 (1919).
Koerner: Gazz. Chim. Ital.
(GCITA9) 4,376 (1874).
Kohn; Pfeifer: Monatsh. Chem. (MOCMB7) 48,236 (1927).
Formulation(s):
eye drops 0.5
%,
1
%;
ophthalmic sol. 10 mglml
Trade Name(s):
D: Iopidine (Alcon) GB: Iopidine (Alcon) USA: Iopidine (Alcon; 1988);
F: Iopidine (Alcon) wfm
Aprindine

ATC: COlBB04
Use: antiarrhythmic
RN: 37640-71-4 MF: CI2,H3,N, MW: 322.50
LD,,: 274 mgkg
(M,
p.0.)
CN:
N-(2,3-dihydro-lH-inden-2-yl)-RP,N-diethyl-N-phenyl-l,3-propanediamine
monohydrochloride
RN: 33237-74-0 MF: CzZH3,N,
.
HCI MW: 358.96 EINECS: 251-418-7
LD,,: 17.1 mglkg (M, i.v.); 262 mglkg (M, p.0.);
16.6 mglkg (R, i.v.); 525 mglkg (R, p.0.)
2-indonone aniline (I) N-(2-indanylidene). 2-anilinoindane (11)
aniline
1.
NaNH2
rCH,
+
1-11
2. J-diethylomino-
propyl chloride
2-indanyl
Aprindine
methonesulfonote
Aprobarbital
A
133
Referenceis):

DE
2
060 721 (Christiaens S. A.; appl. 10.1 2.1970; GB-prior. l9.l2.I968,26.ll.l970).
Formulation(s):
cps. 50 mg; inj. sol. 200 mg120 ml
Trade Name(s):
D: Amidonal (PCR
F:
Fiboran (Nycomed)
Arzneimittel)
I:
Aspenone (Mitsui)
Aprobarbital
ATC: N05CA05
Use: hypnotic, sedative
RN:
77-02- 1 MF: CloH,,N,03 MW: 210.23 EINECS: 200-997-4
LD,,: 200 mgkg (M, i.p.); 350 mgkg (M, s.c.)
CN:
5-(1-methylethyl)-5-(2-propenyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
monosodium salt
RN: 125-88-2 MF: C,,H,,N,NaO, MW: 232.22 EINECS: 204-760-6
LD,,:
85
mgkg (R, i.p.)
5-isoprapyl-
ollyl
bromide
barbituric
acid

I
Aproborbitol
/
Reference(s):
US
1
444
802 (Hoffmann-La Roche; 1923; appl. 1921).
Formulation(s):
elixir 40 mg; tabl. 20 mg, 40 mg, 80 mg
Trade Name(s):
D: Allional (Hoffmann-La Nervisal (Lappe)-comb.; Vita-Dor (Steigerwald).
Roche)-comb.; wfm wfm comb.; wfm
Mandotrilan-"Porte" Nervolitan (Kette1hack)-
USA:
Alurate (Roche); wfm
(Hen@-comb.; wfm comb.; wfm
Nervinum Stada
(Stada)- Resedorm (Lappe)-comb.;
comb.; wfm wfm
Aprotinine
(Trasylol; Triazinin; Zymofren)
ATC: B02AB
Use: proteinase inhibitor, kallikrein
inhibitor
RN: 9087-70-1 MF: C2R4H432N8407YS7 MW: 6511.55 EINECS: 232-904-9
LD,,: >50 ml/kg (M, i.p.); >50 mlkg
(M,
s.c.);
>40 mllkg

(R,
i.p.); >40 mlkg (R, s.c.)
CN:
trypsin inhibitor (ox pancreas basic)
antagosan
RN: 9050-74-2 MF: C284H432N8407YS7 MW: 651 1.55
iniprol
134
A
Aranidipine
ox
pancreas basic
RN: 12407-79-3 MF: C284H4,2N,407,S,
MW:
65 1 1.55
ox
pancreas basic reduced
RN: 11061-94-2 MF: C,,,H4,,N,407,S,
MW:
6517.60
By extraction of animal lymph glands, parotid glands, pancreas, liver, milt and blood serum with dilutcd acetic
acid-ethanol-mixtures upon removal of fat and proteins.
Refererzce(s):
US
2
890 986 (Bayer; 16.6.1959; D-prior. 29.5.1954).
Formulation(s):
amp. 200000 KIU; inj. sol. 100000 KIU/IO ml, 500000 KIU/SO ml
Trade Name(s):
D: Antagosan (Hoechst) Biscol (Lab. Franpis du Trasylol (Bayer)

Beriplast (Centeon
Fractionement ct dcs
J:
Trasylol (Bayer-Yoshitomi;
Pharma)-comb. Biotechno1ogies)-comb. as solution)
Tissucol (Immuno) Trasylol (Bayer-Pharma) USA: Trasylol Injection (Bayer)
Trasylol (Bayer Vital)
I:
Antagosan (Behring)
F:
Antagosan (Hoechst Fase (Astra-Simes)
HoudC) Kir Richter (Lepetit)
Aranidipine
(MPC-
1304)
ATC: C04
Use: antihypertensive, calcium channel
blocker
RN: 86780-90-7
MF:
C,,H,,N207
MW:
388.38
LD,,: 143 mg/kg (M, p.0.);
1459 mgkg (R, p.0.);
3333 mgkg
(dog,
p.0.)
CN:
1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic

acid methyl 2-oxopropyl ester
n
NaH,
benzene
0
diketene 2,2-(ethylene- 2,2-(ethy1enedioxy)-
dioxy)-
1
-propano1 propyl ocetoocetote
(I)
n
H3C
6
,
cH,coou,
benzene
piperidine, acetic acid
2-nitro-
benzoldehyde
2,2-(ethy1enedioxy)-
propyl 2-(2-nitro-
benzy1idene)acetoacetate
(11)
H2N CH
1.
C2H50H,
A
2.
CH,COOH.
H20

I1
+
'(.,
.
CH3
methyl
3-
aminocratonate
Arginine aspartate
A
135
NH,.
CH,OH
CZH50H.
A
I
+
-
Reference(s):
a
Ohno,
S.
eta].: Chem. Pharm. Bull. (CPBTAL) 34(4), 1589-1606 (1986).
b
FR
2 514761 (Maruko Seiyaku; appl. 19.10.1982; J-prior. 19.10.1981).
topical ophthalmic formulation:
WO
9 323 082 (Alcon Lab.; appl. 12.5.1993; USA-prior. 13.5.1992).
Formrrlution(s):

gran.
20
mg/g (2
%)
Trade Name(s):
J: Bec (Maruko; Bristol- Sapresta (Taiho)
Myers Squibb)
Arginine aspartate
ATC: A13A
Use: liver dysfunction therapeutic, tonic
RN:
7675-83-4 MF: C6H14N402 MW: 174.20 EINECS: 231-656-8
CN:
L-aspartic acid compd. with L-arginine (1:l)
H
$2
H2N,,,, COOH
H
N
NdCOOH
+
H
2
HzN,,,
2
-l'
[COOH
NH
Very
pure preparations are obtained by treatment of L-aspartic acid loaded strong basic anion-exchange resins

with an aqueous solution of L-arginine hydrochloride.
L-arginine L-ospartic acid
Reference(s):
DAS
1 518
033
(Mundipharma; appl. 17.9.1965; F-prior. 14.1.1965).
Arginine
asporiate
Formulation(s):
tabl. 1 g; sol. 1 g/10 ml, 1 &/5 ml; tabl.
500
mg, 1 g
Trade Name(s):
D:
Argihepar (Chephasaar);
F:
Sargenor (ASTA Medica)
I:
Glutargin (Terapeutico
wfm M.R.)-comb.
136
A
Arginine pidolate
Sargenor (ASTA Medica)
Arginine pidolate
(Arginine pyroglutamate)
ATC: A13A
Use: tonic, cerebrostimulant
RN: 64855-91-0 MF:

C6H,,N402. C5H,N03 MW: 303.32 EINECS: 265-253-3
CN: 5-0x0-proline compd. with
L-arginine (1: 1)
DL-pyroglutamic L-arginine
acid
Arginine pidolate
DAS
2
416 339 (Manetti Roberts; appl. 4.4.1974; I-prior. 4.4.1973).
GB 1 421 089 (Manetti Roberts; appl. 27.3.1974; I-prior. 4.4.1973).
Provenzano, P.M. et al.:
Arzneim Forsch. (ARZNAD)
27,
1553 (1977).
use as sexual tonic:
DOS 3 125 512
(Manetti Roberts; appl. 29.6.1981; I-prior. 30.6.1980).
Formulation(s):
lyo. 500 mg, 1 g; tabl. 500 mg
Trade Name(s):
I: Adiuvant (Manetti Roberts) Detoxergon Polvere
Detoxergon Fiale (Ba1dacci)-comb.
(Ba1dacci)-comb.
Neoiodarsolo (Ba1dacci)-
comb.
Arotinolol
(S-596)
ATC: C07AA
Use: P-adrenoceptor blocker,
antihypertensive, antianginal

RN: 52560-77-7 MF:
C,~H,,N;O~S~
MW: 37 1.55
LD,,,: >360 mglkg (M, i.p.); 86 mglkg (M, i.v.); >5000 mglkg (M, p.0.)
CN:
5-[2-[[3-[(1,l-dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazo1y1]-2-thiophenecarboxamide
hydrochloride
RN: 80416-73-5 MF: C15H2,N302S,
.
xHC1 MW: unspecified
1.
SOCI,
O
O
Br,.
CH,COOH
1.
thionyl
'~cWNH~
bromine
chloride
5-acetylthiophene-
2-carboxylic acid
Ascorbic
acid
A
137
omrnoniurn
butylornino-
2-rnercopto-4-(5-

dithiocorbomote
2-proponol
corbornoyl-2-thienyl)-
(from tert-butyl-
thiozole
ornine and epi-
chlorohydrin)
Arotinolol
Reference(s):
DOS
2 341 753 (Sumitomo; appl. 17.8.1973; J-prior. 17.8.1972, 5.4.1973).
US
3 932 400 (Sumitomo; 13.1.1976; J-prior. 17.8.1972, 5.4.1973).
Hara,
Y.
et al.: J. Pharm. Sci. (JPMSAE)
67,
1334 (1978).
Formulation(s):
tabl. 10
mg
Trade Narners):
J:
Almarl (Surnitomo; 1986)
Ascorbic acid
(Acide ascorbique;
Vitamin
C)
ATC:
AIlGAOl

Use: antiscorbutical vitamin. antioxidant
RN: 50-81-7 MF: C6H8O6 MW: 176.12 EINECS: 200-066-2
LDS,,:
518rnglkg (M,i.v.); 3367 mg/kg(M,p.o.);
>4
glkg
(R,
i.v.);
11.9
glkg
(R,
p.0.)
CN: I ascorbic acid
monopotassium salt
RN: 15421-15-5 MF: C6H7K06 MW: 214.21 EINECS: 239-432-1
monosodium salt
RN: 134-03-2 MF: C6H7Na0, MW: 198.11 EINECS: 205-126-1
calcium salt
(2:l)
RN: 5743-27-1 MF: C,2Hl,Ca0,, MW: 390.31 EINECS: 227-261-5
magnesium salt
(2:l)
RN: 1543 1-40-0 MF: C,,H,,MgOI2 MW: 374.54 EINECS: 239-442-6
Fe(I1)
salt
(2:l)
RN: 24808-52-4 MF: C,,H,,FeO,, MW: 406.08
Hz.
Roney-Ni
H

,
H:$-~
Acetobocter suboxydons
I
CHO
H
138
A
Ascorbic acid
CH,
acetone diacetone-L-sorbose
CH3
diocetone-2-0x0-
L-gulonic acid
(U)
COOH
ko
2-0x0-L-
gulonic ocid
HO
0
H
Ascorbic ocid
~eichstein,
T.;
Griissner, A.: Helv. Chim. Acta (HCACAV)
17,
31 1 (1934).
Ullmanns Encykl. Tech. Chem., 3. Aufl., Vol. 18,223 ff.
Kirk-Othmer Encycl. Chem. Technol., 2. Ed.

(15SWA8), Vol.
2,
(1963-1971), p. 747 ff.
Formul~ztion(s):
amp. 562 mg; eff. tabl. 1 g; powder 1 g; tabl. 50 mg, 200 mg, 500 mg
Trade Name(s):
Ascorvit (Jenapharm)
Cebion (Merck)
Cetebe
(SmithKline
Beecham)
Cevitt (Hermes)
Vitamin C Phytopharma
(OW)
numerous combination
preparations
Ascofer (Gerda; as iron-
salt)
Laroscorbine
(Roche
Nicholas)
Midy Vitamine C
(SmithKline Beecham)
Vi tascorbol (ThCraplix)
generics (as salts) and
numerous combination
preparations
Ferfolic SV
(Sinc1air)-
comb.

Redoxon (Roche
Consumer)
Acidylina (1st. Italiano
Ferm.)
Agrumina (Also)
Agruvit (Lepetit)
Ascomed (Ripari-Gero)
Ascorgil (Biomedica
Foscama)
Aster C (Corvi)
Bio-Ci (Ceccarelli)
C-Lisa (Lisapharma)
C-Tard (Eurand-Mi)
Cebion (Bracco)
Cecon (Abbott)
Cevit (Italfarmaco)
Duo-C (Geymonat)
Idro-C (Blue Cross)
Lemonvit (Molteni)
Rcdoxon (Roche)
Vicifte (Iacopo Monico)
Vicitina (CT)
Vitamina C Vca
(Bergamon)
Vitamina C Vita
(Synthelabo)
combination preparations
J: Ascoyl (Shionogi); wfm
Hicee (Takeda); wfm
Viscorin (Daiichi); wfm

Vitacimin (Takeda);
wfm
numerous combination
preparations
USA: ACES Antioxidant Soft
Gels (Carlson)
Ce-Vi-Sol (Mead Johnson)
Cevi-Bid (Geriatric
Pharm.)
Chromagen (Savage)
CitraDerm (Pedinol)
Ferancee (Stuart)
Fero-Folic-500 (Abbott)
Fero-Grad-500 (Abbott)
Fetrin (Lunsco)
Irospam (Fielding)
Materna (Lederle Labs.)
Trinsicon
(UCR)
Vi-Daylin ADC (Ross)
Vitron-C (Fisons)
numerous combination
preparations
Asparaginase A
139
Asparaginase
(L-Asparaginase)
ATC: LOIXX; LOlXXO2
Use: antineoplastic
RN: 9015-68-3

MF:
unspecified MW: unspecified EINECS: 232-765-3
LD,,,:
136 glkg
(M,
iv.);
7568 mglkg
(R,
i.v.);
227 mglkg (dog, i.v.)
CN:
asparaginase
L-Asparagine-amidohydrolase.
Relative mol mass 133000
+
5000.
By separation from bacterial culture such as
Escherichia coli, Serratia rnarcescens, Erwinia aroideae, Erwinia
atrosepfica, Erwinia carotovora.
Reference(s):
Ho et
al.:
J. Riol. Chem. (JBCHA3) 245,3708 (1970).
DAS 1 642 615 (Bayer; appl. 27.12.1967).
DAS
1
942
833
(Secret. of Statc for Social Services, London; appl. 22.8.1969; GB-prior. 23.8.1968).
DAS

1
942 900 (Secret. of State for Social Services, London; appl. 22.8.1969; GB-prior. 23.8.1968).
Formulation(s):
inj. powder 10000 iul2.5 ml
Trade Name(s):
D:
Erwinase (Ipsen Pharma)
1:
Crasnitin (Bayer); wfm USA: Elspar (Merck)
F:
Kidrolase (Bellon)
J:
Leunasc (Kyowa Hakko)
Aspartame
LJse: sweetener (pharmaceutical agent)
RN: 22839-47-0
MF:
C,,H,,N,O, MW: 294.31 EINECS: 245-261-3
CN:
N-L-a-aspartyl-L-phenylalanine
1-methyl ester
L-osportic L-aspartic anhydride
acid hydrochlaride
I
Aspartame
(olong
with
aspartame ore formed
up
to

20%
p-isomer.
seporoted
by
crystallization)
Refuence(s):
DE
1 692 768 (Searle
&
Co.; prior. 16.2.1968).
Mazur,
R.H.
et al.: J. Am. Chem. Soc. (JACSA'I')
91,
264 (1969).
Ariyoshi,
Y.
et al.:
Bull.
Chem. Soc. Jpn. (BCSJA8) 46, 1893 (1973).
DE 2 104 620 (Ajinomoto; appl. 1.2.1971; J-prior. 31.1.1970.23.2.1970, 26.6.1970)
DAS 2 152
11 1 (Ajinomoto; appl. 19.10.1971; J-prior. 26.10.1970).
DAS 2
233
535 (Ajinomoto; appl. 7.7.1972; J-prior. 9.7.1972).
US 3 492 131 (Searle; 27.1.1970; appl. 18.4.1966).
140
A
L

-Aspartic acid
alternative synthesis:
US 4 238 392 (Pfizer; 9.12.1980; appl. 29.10.1979).
US 4 173 562 (Monsanto; 6.1 1.1979; prior. 27.12.1976,
3
1.3.1978).
EP 143 881 (Gema; appl. 6.7.1984; CH-prior. 7.9.1983).
,fermentative preparation from
L-aspartic acid
and
L-phenylalanine methyl ester:
US 4 506 011 (Toyo Soda; 19.3.1985; J-prior. 5.9.1981; 14.10.1981, 18.1.1982).
purijication:
US 3 798 207 (Ajinomoto; 19.3.1 974; J-prior. 26.10.1970).
Formulation(s):
eff.
tabl. 20 mg; tabl. 18
mg
Trade Name(s):
D: Canderel (Wander)
F:
Candtrel (Monsanto; 1980)
1:
Aspardolce Dolafic
(Ganassini)
Asparel Dietason
(Formenti)
Aspartina (Ilex)
Bil Aspatame dolaf Hermesetas Gold
(Pietrasanta) (Milanfarma)

Dietoman aspartame Snel Miel (Fea)
(Sterling Midy) Suaviter (Boehringer
Dolcor aspartame Mannh.)
(Gazzoni)
Tac Aspartame (Also)
Futura aspartame J: Pal-Sweet (Ajinomoto)
(Farmacologico Milanese)
L-Aspartic
acid
(L-2-Aminosuccinic acid; Acide aspartique)
Use: non-essential proteinogenic amino
acid (for infusion solutions and
as
salt
former)
RN: 56-84-8 MF: C,H,NO, MW: 133.10 EINECS: 200-291-6
LD,,: 6 glkg (M, i.p.1
CN: L-aspartic acid
monopotassium salt
RN: 11 15-63-5 MF: C4H6KN0, MW: 171.19 EINECS: 214-226-4
monosodium salt
RN: 3792-50-5 MF: C,H,NNaO,
MW:
155.09 EINECS: 223-264-0
magnesium salt
(2:l)
KN:
2068-80-6 MF: C,HI,MgN,O, MW: 288.50 EINECS: 218-191-6
magnesium salt
(2:l)

tetrahydrate
RN: 7018-07-7 MF: C8HL2MgN2O8. 4H20 MW: 360.56
ammonium furnorote
L-hparlic acid
I
Rcference(s):
with immovable aspartase:
Tosa, T. et al.: Biotechnol. Bioeng. (BIBIAU) 15.69 (1973).